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Patent code US10005735

Compile Data Set for Download or QSAR
Found 104 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)		LigandTarget/Host
Links		Ligand
Links		Trg + Lig
Links		Ki
nM		ΔG°
kJ/mole		IC50
nM		Kd
nM		EC50/IC50
nM		koff
s-1		kon
M-1s-1		pHTemp
°C
AMSH-like protease


(Homo sapiens (Human))		BDBM401033
PNG
(US10005735, Compound 31)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCCNC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12 |r|
Show InChI InChI=1S/C23H29N5O3S2/c29-19(8-2-1-7-18-21-16(13-33-18)27-23(31)28-21)24-9-4-10-25-22(30)15-11-14-5-3-6-17(32)20(14)26-12-15/h3,5-6,11-12,16,18,21,32H,1-2,4,7-10,13H2,(H,24,29)(H,25,30)(H2,27,28,31)/t16-,18-,21-/m0/s1
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401008
PNG
(US10005735, Compound 17)
Show SMILES Fc1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C17H13FN2OS/c18-14-6-4-11(5-7-14)9-20-17(21)13-8-12-2-1-3-15(22)16(12)19-10-13/h1-8,10,22H,9H2,(H,20,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401033
PNG
(US10005735, Compound 31)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCCNC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12 |r|
Show InChI InChI=1S/C23H29N5O3S2/c29-19(8-2-1-7-18-21-16(13-33-18)27-23(31)28-21)24-9-4-10-25-22(30)15-11-14-5-3-6-17(32)20(14)26-12-15/h3,5-6,11-12,16,18,21,32H,1-2,4,7-10,13H2,(H,24,29)(H,25,30)(H2,27,28,31)/t16-,18-,21-/m0/s1
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401020
PNG
(US10005735, Compound 19)
Show SMILES COc1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C18H16N2O2S/c1-22-15-7-5-12(6-8-15)10-20-18(21)14-9-13-3-2-4-16(23)17(13)19-11-14/h2-9,11,23H,10H2,1H3,(H,20,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401021
PNG
(US10005735, Compound 20)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccc2OCOc2c1
Show InChI InChI=1S/C18H14N2O3S/c21-18(13-7-12-2-1-3-16(24)17(12)19-9-13)20-8-11-4-5-14-15(6-11)23-10-22-14/h1-7,9,24H,8,10H2,(H,20,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400994
PNG
(US10005735, Compound 7)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccco1
Show InChI InChI=1S/C15H12N2O2S/c18-15(17-9-12-4-2-6-19-12)11-7-10-3-1-5-13(20)14(10)16-8-11/h1-8,20H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401006
PNG
(US10005735, Compound 15)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccncc1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-9-11-4-6-17-7-5-11)13-8-12-2-1-3-14(21)15(12)18-10-13/h1-8,10,21H,9H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400998
PNG
(US10005735, Compound 11)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1cccs1
Show InChI InChI=1S/C16H14N2OS2/c19-16(17-7-6-13-4-2-8-21-13)12-9-11-3-1-5-14(20)15(11)18-10-12/h1-5,8-10,20H,6-7H2,(H,17,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM224012
PNG
(Capzimin | US10005735, Compound 12)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1nccs1
Show InChI InChI=1S/C15H13N3OS2/c19-15(17-5-4-13-16-6-7-21-13)11-8-10-2-1-3-12(20)14(10)18-9-11/h1-3,6-9,20H,4-5H2,(H,17,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401023
PNG
(US10005735, Compound 21)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccc(cc1)N1CCOCC1
Show InChI InChI=1S/C21H21N3O2S/c25-21(17-12-16-2-1-3-19(27)20(16)22-14-17)23-13-15-4-6-18(7-5-15)24-8-10-26-11-9-24/h1-7,12,14,27H,8-11,13H2,(H,23,25)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401034
PNG
(US10005735, Compound 32)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCOCCOCCOCCNC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12 |r|
Show InChI InChI=1S/C28H39N5O6S2/c34-24(7-2-1-6-23-26-21(18-41-23)32-28(36)33-26)29-8-10-37-12-14-39-15-13-38-11-9-30-27(35)20-16-19-4-3-5-22(40)25(19)31-17-20/h3-5,16-17,21,23,26,40H,1-2,6-15,18H2,(H,29,34)(H,30,35)(H2,32,33,36)/t21-,23-,26-/m0/s1
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401034
PNG
(US10005735, Compound 32)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCOCCOCCOCCNC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12 |r|
Show InChI InChI=1S/C28H39N5O6S2/c34-24(7-2-1-6-23-26-21(18-41-23)32-28(36)33-26)29-8-10-37-12-14-39-15-13-38-11-9-30-27(35)20-16-19-4-3-5-22(40)25(19)31-17-20/h3-5,16-17,21,23,26,40H,1-2,6-15,18H2,(H,29,34)(H,30,35)(H2,32,33,36)/t21-,23-,26-/m0/s1
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400992
PNG
(US10005735, Compound 5)
Show SMILES Sc1cccc2cc(cnc12)C(=O)Nc1nccs1
Show InChI InChI=1S/C13H9N3OS2/c17-12(16-13-14-4-5-19-13)9-6-8-2-1-3-10(18)11(8)15-7-9/h1-7,18H,(H,14,16,17)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401029
PNG
(US10005735, Compound 27)
Show SMILES Cc1nc(CCNC(=O)c2cnc3c(S)cccc3c2)sc1C
Show InChI InChI=1S/C17H17N3OS2/c1-10-11(2)23-15(20-10)6-7-18-17(21)13-8-12-4-3-5-14(22)16(12)19-9-13/h3-5,8-9,22H,6-7H2,1-2H3,(H,18,21)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401029
PNG
(US10005735, Compound 27)
Show SMILES Cc1nc(CCNC(=O)c2cnc3c(S)cccc3c2)sc1C
Show InChI InChI=1S/C17H17N3OS2/c1-10-11(2)23-15(20-10)6-7-18-17(21)13-8-12-4-3-5-14(22)16(12)19-9-13/h3-5,8-9,22H,6-7H2,1-2H3,(H,18,21)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401020
PNG
(US10005735, Compound 19)
Show SMILES COc1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C18H16N2O2S/c1-22-15-7-5-12(6-8-15)10-20-18(21)14-9-13-3-2-4-16(23)17(13)19-11-14/h2-9,11,23H,10H2,1H3,(H,20,21)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400996
PNG
(US10005735, Compound 9)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1nccs1
Show InChI InChI=1S/C14H11N3OS2/c18-14(17-8-12-15-4-5-20-12)10-6-9-2-1-3-11(19)13(9)16-7-10/h1-7,19H,8H2,(H,17,18)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401006
PNG
(US10005735, Compound 15)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccncc1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-9-11-4-6-17-7-5-11)13-8-12-2-1-3-14(21)15(12)18-10-13/h1-8,10,21H,9H2,(H,19,20)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401020
PNG
(US10005735, Compound 19)
Show SMILES COc1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C18H16N2O2S/c1-22-15-7-5-12(6-8-15)10-20-18(21)14-9-13-3-2-4-16(23)17(13)19-11-14/h2-9,11,23H,10H2,1H3,(H,20,21)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401026
PNG
(US10005735, Compound 24)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCCc1cccs1
Show InChI InChI=1S/C16H14N2OS2/c19-16(18-8-6-11-3-2-10-21-11)13-7-9-17-15-12(13)4-1-5-14(15)20/h1-5,7,9-10,20H,6,8H2,(H,18,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401030
PNG
(US10005735, Compound 28)
Show SMILES CCOC(=O)c1csc(CCNC(=O)c2cnc3c(S)cccc3c2)n1
Show InChI InChI=1S/C18H17N3O3S2/c1-2-24-18(23)13-10-26-15(21-13)6-7-19-17(22)12-8-11-4-3-5-14(25)16(11)20-9-12/h3-5,8-10,25H,2,6-7H2,1H3,(H,19,22)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401009
PNG
(US10005735, Compound 18)
Show SMILES FC(F)(F)c1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C18H13F3N2OS/c19-18(20,21)14-6-4-11(5-7-14)9-23-17(24)13-8-12-2-1-3-15(25)16(12)22-10-13/h1-8,10,25H,9H2,(H,23,24)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401030
PNG
(US10005735, Compound 28)
Show SMILES CCOC(=O)c1csc(CCNC(=O)c2cnc3c(S)cccc3c2)n1
Show InChI InChI=1S/C18H17N3O3S2/c1-2-24-18(23)13-10-26-15(21-13)6-7-19-17(22)12-8-11-4-3-5-14(25)16(11)20-9-12/h3-5,8-10,25H,2,6-7H2,1H3,(H,19,22)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401023
PNG
(US10005735, Compound 21)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccc(cc1)N1CCOCC1
Show InChI InChI=1S/C21H21N3O2S/c25-21(17-12-16-2-1-3-19(27)20(16)22-14-17)23-13-15-4-6-18(7-5-15)24-8-10-26-11-9-24/h1-7,12,14,27H,8-11,13H2,(H,23,25)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400995
PNG
(US10005735, Compound 8)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1cccs1
Show InChI InChI=1S/C15H12N2OS2/c18-15(17-9-12-4-2-6-20-12)11-7-10-3-1-5-13(19)14(10)16-8-11/h1-8,19H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401031
PNG
(US10005735, Compound 29)
Show SMILES Cc1nc(CCNC(=O)c2cnc3c(S)cccc3c2)sc1C(O)=O
Show InChI InChI=1S/C17H15N3O3S2/c1-9-15(17(22)23)25-13(20-9)5-6-18-16(21)11-7-10-3-2-4-12(24)14(10)19-8-11/h2-4,7-8,24H,5-6H2,1H3,(H,18,21)(H,22,23)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401008
PNG
(US10005735, Compound 17)
Show SMILES Fc1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C17H13FN2OS/c18-14-6-4-11(5-7-14)9-20-17(21)13-8-12-2-1-3-15(22)16(12)19-10-13/h1-8,10,22H,9H2,(H,20,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401023
PNG
(US10005735, Compound 21)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccc(cc1)N1CCOCC1
Show InChI InChI=1S/C21H21N3O2S/c25-21(17-12-16-2-1-3-19(27)20(16)22-14-17)23-13-15-4-6-18(7-5-15)24-8-10-26-11-9-24/h1-7,12,14,27H,8-11,13H2,(H,23,25)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400994
PNG
(US10005735, Compound 7)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccco1
Show InChI InChI=1S/C15H12N2O2S/c18-15(17-9-12-4-2-6-19-12)11-7-10-3-1-5-13(20)14(10)16-8-11/h1-8,20H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400994
PNG
(US10005735, Compound 7)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccco1
Show InChI InChI=1S/C15H12N2O2S/c18-15(17-9-12-4-2-6-19-12)11-7-10-3-1-5-13(20)14(10)16-8-11/h1-8,20H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401021
PNG
(US10005735, Compound 20)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccc2OCOc2c1
Show InChI InChI=1S/C18H14N2O3S/c21-18(13-7-12-2-1-3-16(24)17(12)19-9-13)20-8-11-4-5-14-15(6-11)23-10-22-14/h1-7,9,24H,8,10H2,(H,20,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401026
PNG
(US10005735, Compound 24)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCCc1cccs1
Show InChI InChI=1S/C16H14N2OS2/c19-16(18-8-6-11-3-2-10-21-11)13-7-9-17-15-12(13)4-1-5-14(15)20/h1-5,7,9-10,20H,6,8H2,(H,18,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401028
PNG
(US10005735, Compound 26)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCCc1ccco1
Show InChI InChI=1S/C16H14N2O2S/c19-16(18-8-6-11-3-2-10-20-11)13-7-9-17-15-12(13)4-1-5-14(15)21/h1-5,7,9-10,21H,6,8H2,(H,18,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400988
PNG
(US10005735, Compound 1)
Show SMILES NC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C10H8N2OS/c11-10(13)7-4-6-2-1-3-8(14)9(6)12-5-7/h1-5,14H,(H2,11,13)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401031
PNG
(US10005735, Compound 29)
Show SMILES Cc1nc(CCNC(=O)c2cnc3c(S)cccc3c2)sc1C(O)=O
Show InChI InChI=1S/C17H15N3O3S2/c1-9-15(17(22)23)25-13(20-9)5-6-18-16(21)11-7-10-3-2-4-12(24)14(10)19-8-11/h2-4,7-8,24H,5-6H2,1H3,(H,18,21)(H,22,23)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401007
PNG
(US10005735, Compound 16)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccccc1
Show InChI InChI=1S/C17H14N2OS/c20-17(19-10-12-5-2-1-3-6-12)14-9-13-7-4-8-15(21)16(13)18-11-14/h1-9,11,21H,10H2,(H,19,20)
PDB

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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400988
PNG
(US10005735, Compound 1)
Show SMILES NC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C10H8N2OS/c11-10(13)7-4-6-2-1-3-8(14)9(6)12-5-7/h1-5,14H,(H2,11,13)
PDB

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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401025
PNG
(US10005735, Compound 23)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCc1cccs1
Show InChI InChI=1S/C15H12N2OS2/c18-15(17-9-10-3-2-8-20-10)12-6-7-16-14-11(12)4-1-5-13(14)19/h1-8,19H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400997
PNG
(US10005735, Compound 10)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1ccco1
Show InChI InChI=1S/C16H14N2O2S/c19-16(17-7-6-13-4-2-8-20-13)12-9-11-3-1-5-14(21)15(11)18-10-12/h1-5,8-10,21H,6-7H2,(H,17,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400998
PNG
(US10005735, Compound 11)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1cccs1
Show InChI InChI=1S/C16H14N2OS2/c19-16(17-7-6-13-4-2-8-21-13)12-9-11-3-1-5-14(20)15(11)18-10-12/h1-5,8-10,20H,6-7H2,(H,17,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400995
PNG
(US10005735, Compound 8)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1cccs1
Show InChI InChI=1S/C15H12N2OS2/c18-15(17-9-12-4-2-6-20-12)11-7-10-3-1-5-13(19)14(10)16-8-11/h1-8,19H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400989
PNG
(US10005735, Compound 2)
Show SMILES CNC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C11H10N2OS/c1-12-11(14)8-5-7-3-2-4-9(15)10(7)13-6-8/h2-6,15H,1H3,(H,12,14)
PDB

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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400997
PNG
(US10005735, Compound 10)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1ccco1
Show InChI InChI=1S/C16H14N2O2S/c19-16(17-7-6-13-4-2-8-20-13)12-9-11-3-1-5-14(21)15(11)18-10-12/h1-5,8-10,21H,6-7H2,(H,17,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401027
PNG
(US10005735, Compound 25)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCc1ccco1
Show InChI InChI=1S/C15H12N2O2S/c18-15(17-9-10-3-2-8-19-10)12-6-7-16-14-11(12)4-1-5-13(14)20/h1-8,20H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401027
PNG
(US10005735, Compound 25)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCc1ccco1
Show InChI InChI=1S/C15H12N2O2S/c18-15(17-9-10-3-2-8-19-10)12-6-7-16-14-11(12)4-1-5-13(14)20/h1-8,20H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400990
PNG
(US10005735, Compound 3)
Show SMILES COC(=O)CNC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C13H12N2O3S/c1-18-11(16)7-15-13(17)9-5-8-3-2-4-10(19)12(8)14-6-9/h2-6,19H,7H2,1H3,(H,15,17)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401025
PNG
(US10005735, Compound 23)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCc1cccs1
Show InChI InChI=1S/C15H12N2OS2/c18-15(17-9-10-3-2-8-20-10)12-6-7-16-14-11(12)4-1-5-13(14)19/h1-8,19H,9H2,(H,17,18)
PDB

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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400991
PNG
(US10005735, Compound 4)
Show SMILES Sc1cccc2cc(cnc12)C(=O)Nc1ncco1
Show InChI InChI=1S/C13H9N3O2S/c17-12(16-13-14-4-5-18-13)9-6-8-2-1-3-10(19)11(8)15-7-9/h1-7,19H,(H,14,16,17)
PDB

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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400990
PNG
(US10005735, Compound 3)
Show SMILES COC(=O)CNC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C13H12N2O3S/c1-18-11(16)7-15-13(17)9-5-8-3-2-4-10(19)12(8)14-6-9/h2-6,19H,7H2,1H3,(H,15,17)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM224013
PNG
(8-Mercaptoquinoline (8TQ) | US10005735, Example 8T...)
Show SMILES Sc1cccc2cccnc12
Show InChI InChI=1S/C9H7NS/c11-8-5-1-3-7-4-2-6-10-9(7)8/h1-6,11H
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401028
PNG
(US10005735, Compound 26)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCCc1ccco1
Show InChI InChI=1S/C16H14N2O2S/c19-16(18-8-6-11-3-2-10-20-11)13-7-9-17-15-12(13)4-1-5-14(15)21/h1-5,7,9-10,21H,6,8H2,(H,18,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401005
PNG
(US10005735, Compound 14)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1cccnc1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-9-11-3-2-6-17-8-11)13-7-12-4-1-5-14(21)15(12)18-10-13/h1-8,10,21H,9H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400992
PNG
(US10005735, Compound 5)
Show SMILES Sc1cccc2cc(cnc12)C(=O)Nc1nccs1
Show InChI InChI=1S/C13H9N3OS2/c17-12(16-13-14-4-5-19-13)9-6-8-2-1-3-10(18)11(8)15-7-9/h1-7,18H,(H,14,16,17)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401009
PNG
(US10005735, Compound 18)
Show SMILES FC(F)(F)c1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C18H13F3N2OS/c19-18(20,21)14-6-4-11(5-7-14)9-23-17(24)13-8-12-2-1-3-15(25)16(12)22-10-13/h1-8,10,25H,9H2,(H,23,24)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401005
PNG
(US10005735, Compound 14)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1cccnc1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-9-11-3-2-6-17-8-11)13-7-12-4-1-5-14(21)15(12)18-10-13/h1-8,10,21H,9H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401004
PNG
(US10005735, Compound 13)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccccn1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-10-13-5-1-2-7-17-13)12-8-11-4-3-6-14(21)15(11)18-9-12/h1-9,21H,10H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400998
PNG
(US10005735, Compound 11)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1cccs1
Show InChI InChI=1S/C16H14N2OS2/c19-16(17-7-6-13-4-2-8-21-13)12-9-11-3-1-5-14(20)15(11)18-10-12/h1-5,8-10,20H,6-7H2,(H,17,19)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401029
PNG
(US10005735, Compound 27)
Show SMILES Cc1nc(CCNC(=O)c2cnc3c(S)cccc3c2)sc1C
Show InChI InChI=1S/C17H17N3OS2/c1-10-11(2)23-15(20-10)6-7-18-17(21)13-8-12-4-3-5-14(22)16(12)19-9-13/h3-5,8-9,22H,6-7H2,1-2H3,(H,18,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM224012
PNG
(Capzimin | US10005735, Compound 12)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1nccs1
Show InChI InChI=1S/C15H13N3OS2/c19-15(17-5-4-13-16-6-7-21-13)11-8-10-2-1-3-12(20)14(10)18-9-11/h1-3,6-9,20H,4-5H2,(H,17,19)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM400993
PNG
(US10005735, Compound 6)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCC1CCCO1
Show InChI InChI=1S/C15H16N2O2S/c18-15(17-9-12-4-2-6-19-12)11-7-10-3-1-5-13(20)14(10)16-8-11/h1,3,5,7-8,12,20H,2,4,6,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400989
PNG
(US10005735, Compound 2)
Show SMILES CNC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C11H10N2OS/c1-12-11(14)8-5-7-3-2-4-9(15)10(7)13-6-8/h2-6,15H,1H3,(H,12,14)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401027
PNG
(US10005735, Compound 25)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCc1ccco1
Show InChI InChI=1S/C15H12N2O2S/c18-15(17-9-10-3-2-8-19-10)12-6-7-16-14-11(12)4-1-5-13(14)20/h1-8,20H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400991
PNG
(US10005735, Compound 4)
Show SMILES Sc1cccc2cc(cnc12)C(=O)Nc1ncco1
Show InChI InChI=1S/C13H9N3O2S/c17-12(16-13-14-4-5-18-13)9-6-8-2-1-3-10(19)11(8)15-7-9/h1-7,19H,(H,14,16,17)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401024
PNG
(US10005735, Compound 22)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCN1CCOCC1
Show InChI InChI=1S/C16H19N3O2S/c20-16(17-4-5-19-6-8-21-9-7-19)13-10-12-2-1-3-14(22)15(12)18-11-13/h1-3,10-11,22H,4-9H2,(H,17,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400993
PNG
(US10005735, Compound 6)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCC1CCCO1
Show InChI InChI=1S/C15H16N2O2S/c18-15(17-9-12-4-2-6-19-12)11-7-10-3-1-5-13(20)14(10)16-8-11/h1,3,5,7-8,12,20H,2,4,6,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400997
PNG
(US10005735, Compound 10)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1ccco1
Show InChI InChI=1S/C16H14N2O2S/c19-16(17-7-6-13-4-2-8-20-13)12-9-11-3-1-5-14(21)15(11)18-10-12/h1-5,8-10,21H,6-7H2,(H,17,19)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401006
PNG
(US10005735, Compound 15)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccncc1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-9-11-4-6-17-7-5-11)13-8-12-2-1-3-14(21)15(12)18-10-13/h1-8,10,21H,9H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401021
PNG
(US10005735, Compound 20)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccc2OCOc2c1
Show InChI InChI=1S/C18H14N2O3S/c21-18(13-7-12-2-1-3-16(24)17(12)19-9-13)20-8-11-4-5-14-15(6-11)23-10-22-14/h1-7,9,24H,8,10H2,(H,20,21)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401026
PNG
(US10005735, Compound 24)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCCc1cccs1
Show InChI InChI=1S/C16H14N2OS2/c19-16(18-8-6-11-3-2-10-21-11)13-7-9-17-15-12(13)4-1-5-14(15)20/h1-5,7,9-10,20H,6,8H2,(H,18,19)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401033
PNG
(US10005735, Compound 31)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCCNC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12 |r|
Show InChI InChI=1S/C23H29N5O3S2/c29-19(8-2-1-7-18-21-16(13-33-18)27-23(31)28-21)24-9-4-10-25-22(30)15-11-14-5-3-6-17(32)20(14)26-12-15/h3,5-6,11-12,16,18,21,32H,1-2,4,7-10,13H2,(H,24,29)(H,25,30)(H2,27,28,31)/t16-,18-,21-/m0/s1
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM400996
PNG
(US10005735, Compound 9)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1nccs1
Show InChI InChI=1S/C14H11N3OS2/c18-14(17-8-12-15-4-5-20-12)10-6-9-2-1-3-11(19)13(9)16-7-10/h1-7,19H,8H2,(H,17,18)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401028
PNG
(US10005735, Compound 26)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCCc1ccco1
Show InChI InChI=1S/C16H14N2O2S/c19-16(18-8-6-11-3-2-10-20-11)13-7-9-17-15-12(13)4-1-5-14(15)21/h1-5,7,9-10,21H,6,8H2,(H,18,19)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401007
PNG
(US10005735, Compound 16)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccccc1
Show InChI InChI=1S/C17H14N2OS/c20-17(19-10-12-5-2-1-3-6-12)14-9-13-7-4-8-15(21)16(13)18-11-14/h1-9,11,21H,10H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM401032
PNG
(US10005735, Compound 30)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1nc(cs1)-c1ccccc1
Show InChI InChI=1S/C21H17N3OS2/c25-21(16-11-15-7-4-8-18(26)20(15)23-12-16)22-10-9-19-24-17(13-27-19)14-5-2-1-3-6-14/h1-8,11-13,26H,9-10H2,(H,22,25)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401034
PNG
(US10005735, Compound 32)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCOCCOCCOCCNC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12 |r|
Show InChI InChI=1S/C28H39N5O6S2/c34-24(7-2-1-6-23-26-21(18-41-23)32-28(36)33-26)29-8-10-37-12-14-39-15-13-38-11-9-30-27(35)20-16-19-4-3-5-22(40)25(19)31-17-20/h3-5,16-17,21,23,26,40H,1-2,6-15,18H2,(H,29,34)(H,30,35)(H2,32,33,36)/t21-,23-,26-/m0/s1
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM50264563
PNG
(CHEMBL4069573 | US10005735, Table 1.8)
Show SMILES Sc1ccnc2cccnc12
Show InChI InChI=1S/C8H6N2S/c11-7-3-5-9-6-2-1-4-10-8(6)7/h1-5H,(H,9,11)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400991
PNG
(US10005735, Compound 4)
Show SMILES Sc1cccc2cc(cnc12)C(=O)Nc1ncco1
Show InChI InChI=1S/C13H9N3O2S/c17-12(16-13-14-4-5-18-13)9-6-8-2-1-3-10(19)11(8)15-7-9/h1-7,19H,(H,14,16,17)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400988
PNG
(US10005735, Compound 1)
Show SMILES NC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C10H8N2OS/c11-10(13)7-4-6-2-1-3-8(14)9(6)12-5-7/h1-5,14H,(H2,11,13)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401007
PNG
(US10005735, Compound 16)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccccc1
Show InChI InChI=1S/C17H14N2OS/c20-17(19-10-12-5-2-1-3-6-12)14-9-13-7-4-8-15(21)16(13)18-11-14/h1-9,11,21H,10H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400995
PNG
(US10005735, Compound 8)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1cccs1
Show InChI InChI=1S/C15H12N2OS2/c18-15(17-9-12-4-2-6-20-12)11-7-10-3-1-5-13(19)14(10)16-8-11/h1-8,19H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401004
PNG
(US10005735, Compound 13)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccccn1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-10-13-5-1-2-7-17-13)12-8-11-4-3-6-14(21)15(11)18-9-12/h1-9,21H,10H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401008
PNG
(US10005735, Compound 17)
Show SMILES Fc1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C17H13FN2OS/c18-14-6-4-11(5-7-14)9-20-17(21)13-8-12-2-1-3-15(22)16(12)19-10-13/h1-8,10,22H,9H2,(H,20,21)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401025
PNG
(US10005735, Compound 23)
Show SMILES Sc1cccc2c(ccnc12)C(=O)NCc1cccs1
Show InChI InChI=1S/C15H12N2OS2/c18-15(17-9-10-3-2-8-20-10)12-6-7-16-14-11(12)4-1-5-13(14)19/h1-8,19H,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401030
PNG
(US10005735, Compound 28)
Show SMILES CCOC(=O)c1csc(CCNC(=O)c2cnc3c(S)cccc3c2)n1
Show InChI InChI=1S/C18H17N3O3S2/c1-2-24-18(23)13-10-26-15(21-13)6-7-19-17(22)12-8-11-4-3-5-14(25)16(11)20-9-12/h3-5,8-10,25H,2,6-7H2,1H3,(H,19,22)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401031
PNG
(US10005735, Compound 29)
Show SMILES Cc1nc(CCNC(=O)c2cnc3c(S)cccc3c2)sc1C(O)=O
Show InChI InChI=1S/C17H15N3O3S2/c1-9-15(17(22)23)25-13(20-9)5-6-18-16(21)11-7-10-3-2-4-12(24)14(10)19-8-11/h2-4,7-8,24H,5-6H2,1H3,(H,18,21)(H,22,23)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400996
PNG
(US10005735, Compound 9)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1nccs1
Show InChI InChI=1S/C14H11N3OS2/c18-14(17-8-12-15-4-5-20-12)10-6-9-2-1-3-11(19)13(9)16-7-10/h1-7,19H,8H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401024
PNG
(US10005735, Compound 22)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCN1CCOCC1
Show InChI InChI=1S/C16H19N3O2S/c20-16(17-4-5-19-6-8-21-9-7-19)13-10-12-2-1-3-14(22)15(12)18-11-13/h1-3,10-11,22H,4-9H2,(H,17,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM224012
PNG
(Capzimin | US10005735, Compound 12)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1nccs1
Show InChI InChI=1S/C15H13N3OS2/c19-15(17-5-4-13-16-6-7-21-13)11-8-10-2-1-3-12(20)14(10)18-9-11/h1-3,6-9,20H,4-5H2,(H,17,19)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400992
PNG
(US10005735, Compound 5)
Show SMILES Sc1cccc2cc(cnc12)C(=O)Nc1nccs1
Show InChI InChI=1S/C13H9N3OS2/c17-12(16-13-14-4-5-19-13)9-6-8-2-1-3-10(18)11(8)15-7-9/h1-7,18H,(H,14,16,17)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401032
PNG
(US10005735, Compound 30)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1nc(cs1)-c1ccccc1
Show InChI InChI=1S/C21H17N3OS2/c25-21(16-11-15-7-4-8-18(26)20(15)23-12-16)22-10-9-19-24-17(13-27-19)14-5-2-1-3-6-14/h1-8,11-13,26H,9-10H2,(H,22,25)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400993
PNG
(US10005735, Compound 6)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCC1CCCO1
Show InChI InChI=1S/C15H16N2O2S/c18-15(17-9-12-4-2-6-19-12)11-7-10-3-1-5-13(20)14(10)16-8-11/h1,3,5,7-8,12,20H,2,4,6,9H2,(H,17,18)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401004
PNG
(US10005735, Compound 13)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1ccccn1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-10-13-5-1-2-7-17-13)12-8-11-4-3-6-14(21)15(11)18-9-12/h1-9,21H,10H2,(H,19,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400989
PNG
(US10005735, Compound 2)
Show SMILES CNC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C11H10N2OS/c1-12-11(14)8-5-7-3-2-4-9(15)10(7)13-6-8/h2-6,15H,1H3,(H,12,14)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401024
PNG
(US10005735, Compound 22)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCN1CCOCC1
Show InChI InChI=1S/C16H19N3O2S/c20-16(17-4-5-19-6-8-21-9-7-19)13-10-12-2-1-3-14(22)15(12)18-11-13/h1-3,10-11,22H,4-9H2,(H,17,20)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM50264546
PNG
(CHEMBL4094874 | US10005735, Table 1.3)
Show SMILES Sc1cccc2ccccc12
Show InChI InChI=1S/C10H8S/c11-10-7-3-5-8-4-1-2-6-9(8)10/h1-7,11H
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM32144
PNG
(8-quinolinamine | 8-quinolylamine | AS-232 | US100...)
Show SMILES Nc1cccc2cccnc12
Show InChI InChI=1S/C9H8N2/c10-8-5-1-3-7-4-2-6-11-9(7)8/h1-6H,10H2
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM50264534
PNG
(CHEMBL4075311 | US10005735, Table 1.6)
Show SMILES Sc1cccc2ncccc12
Show InChI InChI=1S/C9H7NS/c11-9-5-1-4-8-7(9)3-2-6-10-8/h1-6,11H
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401009
PNG
(US10005735, Compound 18)
Show SMILES FC(F)(F)c1ccc(CNC(=O)c2cnc3c(S)cccc3c2)cc1
Show InChI InChI=1S/C18H13F3N2OS/c19-18(20,21)14-6-4-11(5-7-14)9-23-17(24)13-8-12-2-1-3-15(25)16(12)22-10-13/h1-8,10,25H,9H2,(H,23,24)
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM50264545
PNG
(CHEBI:48984 | CHEMBL1702610 | US10005735, Table 1....)
Show SMILES Cc1cccc2cccnc12
Show InChI InChI=1S/C10H9N/c1-8-4-2-5-9-6-3-7-11-10(8)9/h2-7H,1H3
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Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM32203
PNG
(8-quinolinol | CHEMBL310555 | US10005735, Table 1....)
Show SMILES Oc1cccc2cccnc12
Show InChI InChI=1S/C9H7NO/c11-8-5-1-3-7-4-2-6-10-9(7)8/h1-6,11H
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
26S proteasome non-ATPase regulatory subunit 14


(Homo sapiens (Human))		BDBM50264536
PNG
(CHEMBL4076981 | US10005735, Table 1.4)
Show SMILES CSc1cccc2cccnc12
Show InChI InChI=1S/C10H9NS/c1-12-9-6-2-4-8-5-3-7-11-10(8)9/h2-7H,1H3
PDB

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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
AMSH-like protease


(Homo sapiens (Human))		BDBM401032
PNG
(US10005735, Compound 30)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCCc1nc(cs1)-c1ccccc1
Show InChI InChI=1S/C21H17N3OS2/c25-21(16-11-15-7-4-8-18(26)20(15)23-12-16)22-10-9-19-24-17(13-27-19)14-5-2-1-3-6-14/h1-8,11-13,26H,9-10H2,(H,22,25)
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Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM400990
PNG
(US10005735, Compound 3)
Show SMILES COC(=O)CNC(=O)c1cnc2c(S)cccc2c1
Show InChI InChI=1S/C13H12N2O3S/c1-18-11(16)7-15-13(17)9-5-8-3-2-4-10(19)12(8)14-6-9/h2-6,19H,7H2,1H3,(H,15,17)
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n/an/a 1.20E+5n/an/an/an/an/an/a



Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM401005
PNG
(US10005735, Compound 14)
Show SMILES Sc1cccc2cc(cnc12)C(=O)NCc1cccnc1
Show InChI InChI=1S/C16H13N3OS/c20-16(19-9-11-3-2-6-17-8-11)13-7-12-4-1-5-14(21)15(12)18-10-13/h1-8,10,21H,9H2,(H,19,20)
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n/an/a 1.28E+5n/an/an/an/an/an/a



Wyeth Research



Assay Description
In brief, this Rpn11 bioassay employs a fluorescent polarization readout based on the ability of the 26S proteasome to cleave the protein substrate i...

Bioorg Med Chem 17: 8086-92 (2009)


BindingDB Entry DOI: 10.7270/Q22R3V09
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%