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Compile Data Set for Download or QSAR

Found 68 hits Enz. Inhib. hit(s) with Target = 'COP9 signalosome complex subunit 5'   
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
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50514114
PNG
(CHEMBL4528101)
Show SMILES CC(C)n1nc(cc1C(=O)Nc1ccc([C@H]2[C@@H](O)CCCc3cncn23)c(c1)-c1ccccc1)C(F)F |r|
Show InChI InChI=1S/C28H29F2N5O2/c1-17(2)35-24(14-23(33-35)27(29)30)28(37)32-19-11-12-21(22(13-19)18-7-4-3-5-8-18)26-25(36)10-6-9-20-15-31-16-34(20)26/h3-5,7-8,11-17,25-27,36H,6,9-10H2,1-2H3,(H,32,37)/t25-,26-/m0/s1
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n/an/a 5.80n/an/an/an/an/an/a



Dana-Farber Cancer Institute

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using fluorescence-labeled CRL substrate by TR-FRET assay

J Med Chem 63: 2731-2750 (2020)


Article DOI: 10.1021/acs.jmedchem.9b01138
BindingDB Entry DOI: 10.7270/Q2GF0XTC
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50514115
PNG
(CHEMBL4447716)
Show SMILES Cc1ccc(-c2[nH]c3ncccc3c2CCC(=O)N2CCOC[C@H]2c2nc3ccccc3[nH]2)c(c1)-c1ccccc1 |r|
Show InChI InChI=1S/C34H31N5O2/c1-22-13-14-25(27(20-22)23-8-3-2-4-9-23)32-24(26-10-7-17-35-33(26)38-32)15-16-31(40)39-18-19-41-21-30(39)34-36-28-11-5-6-12-29(28)37-34/h2-14,17,20,30H,15-16,18-19,21H2,1H3,(H,35,38)(H,36,37)/t30-/m0/s1
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n/an/a 60n/an/an/an/an/an/a



Dana-Farber Cancer Institute

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using fluorescence-labeled CRL substrate by TR-FRET assay

J Med Chem 63: 2731-2750 (2020)


Article DOI: 10.1021/acs.jmedchem.9b01138
BindingDB Entry DOI: 10.7270/Q2GF0XTC
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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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n/an/a 200n/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))		BDBM50264453
PNG
(CHEMBL4088568)
Show SMILES O=C(NCc1ccc(cc1)N1CCCCC1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3ccc(cc3)N3CCOCC3)cccc2c1
Show InChI InChI=1S/C43H42N6O3S2/c50-42(46-26-30-10-14-36(15-11-30)48-18-2-1-3-19-48)34-24-32-6-4-8-38(40(32)44-28-34)53-54-39-9-5-7-33-25-35(29-45-41(33)39)43(51)47-27-31-12-16-37(17-13-31)49-20-22-52-23-21-49/h4-17,24-25,28-29H,1-3,18-23,26-27H2,(H,46,50)(H,47,51)
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n/an/a 300n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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
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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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))		BDBM50264426
PNG
(CHEMBL4095913)
Show SMILES O=C(NCc1ccco1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3ccco3)cccc2c1
Show InChI InChI=1S/C30H22N4O4S2/c35-29(33-17-23-7-3-11-37-23)21-13-19-5-1-9-25(27(19)31-15-21)39-40-26-10-2-6-20-14-22(16-32-28(20)26)30(36)34-18-24-8-4-12-38-24/h1-16H,17-18H2,(H,33,35)(H,34,36)
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n/an/a<500n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264415
PNG
(CHEMBL4096289)
Show SMILES COc1ccc(CNC(=O)c2cnc3c(SSc4cccc5cc(cnc45)C(=O)NCc4ccc(OC)cc4)cccc3c2)cc1
Show InChI InChI=1S/C36H30N4O4S2/c1-43-29-13-9-23(10-14-29)19-39-35(41)27-17-25-5-3-7-31(33(25)37-21-27)45-46-32-8-4-6-26-18-28(22-38-34(26)32)36(42)40-20-24-11-15-30(44-2)16-12-24/h3-18,21-22H,19-20H2,1-2H3,(H,39,41)(H,40,42)
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n/an/a 500n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264491
PNG
(CHEMBL4101230)
Show SMILES Cc1cc(S)c2ncccc2c1
Show InChI InChI=1S/C10H9NS/c1-7-5-8-3-2-4-11-10(8)9(12)6-7/h2-6,12H,1H3
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n/an/a 1.60E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264484
PNG
(CHEMBL4084782)
Show SMILES Cc1ccc(S)c2ncccc12
Show InChI InChI=1S/C10H9NS/c1-7-4-5-9(12)10-8(7)3-2-6-11-10/h2-6,12H,1H3
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n/an/a 2.90E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264420
PNG
(CHEMBL4100384)
Show SMILES O=C(NCCc1cccs1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCCc3cccs3)cccc2c1
Show InChI InChI=1S/C32H26N4O2S4/c37-31(33-13-11-25-7-3-15-39-25)23-17-21-5-1-9-27(29(21)35-19-23)41-42-28-10-2-6-22-18-24(20-36-30(22)28)32(38)34-14-12-26-8-4-16-40-26/h1-10,15-20H,11-14H2,(H,33,37)(H,34,38)
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n/an/a 4.00E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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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))		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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n/an/a 4.40E+3n/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))		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
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264421
PNG
(CHEMBL4099434)
Show SMILES O=C(NCCc1ccco1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCCc3ccco3)cccc2c1
Show InChI InChI=1S/C32H26N4O4S2/c37-31(33-13-11-25-7-3-15-39-25)23-17-21-5-1-9-27(29(21)35-19-23)41-42-28-10-2-6-22-18-24(20-36-30(22)28)32(38)34-14-12-26-8-4-16-40-26/h1-10,15-20H,11-14H2,(H,33,37)(H,34,38)
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n/an/a 6.90E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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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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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))		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))		BDBM50264417
PNG
(CHEMBL4104719)
Show SMILES O=C(NCc1ccncc1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3ccncc3)cccc2c1
Show InChI InChI=1S/C32H24N6O2S2/c39-31(37-17-21-7-11-33-12-8-21)25-15-23-3-1-5-27(29(23)35-19-25)41-42-28-6-2-4-24-16-26(20-36-30(24)28)32(40)38-18-22-9-13-34-14-10-22/h1-16,19-20H,17-18H2,(H,37,39)(H,38,40)
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n/an/a 7.00E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264455
PNG
(CHEMBL4060337)
Show SMILES O=C(NCc1ccc2OCOc2c1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3ccc4OCOc4c3)cccc2c1
Show InChI InChI=1S/C36H26N4O6S2/c41-35(39-15-21-7-9-27-29(11-21)45-19-43-27)25-13-23-3-1-5-31(33(23)37-17-25)47-48-32-6-2-4-24-14-26(18-38-34(24)32)36(42)40-16-22-8-10-28-30(12-22)46-20-44-28/h1-14,17-18H,15-16,19-20H2,(H,39,41)(H,40,42)
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n/an/a 7.00E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264503
PNG
(CHEMBL4100994)
Show SMILES Cc1cnc2c(S)cccc2c1
Show InChI InChI=1S/C10H9NS/c1-7-5-8-3-2-4-9(12)10(8)11-6-7/h2-6,12H,1H3
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n/an/a 7.10E+3n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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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))		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
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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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))		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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n/an/a 1.03E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264425
PNG
(CHEMBL4095417)
Show SMILES O=C(NCc1ccccc1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3ccccc3)cccc2c1
Show InChI InChI=1S/C34H26N4O2S2/c39-33(37-19-23-9-3-1-4-10-23)27-17-25-13-7-15-29(31(25)35-21-27)41-42-30-16-8-14-26-18-28(22-36-32(26)30)34(40)38-20-24-11-5-2-6-12-24/h1-18,21-22H,19-20H2,(H,37,39)(H,38,40)
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University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264481
PNG
(CHEMBL4065318)
Show SMILES O=C(Nc1ncco1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)Nc3ncco3)cccc2c1
Show InChI InChI=1S/C26H16N6O4S2/c33-23(31-25-27-7-9-35-25)17-11-15-3-1-5-19(21(15)29-13-17)37-38-20-6-2-4-16-12-18(14-30-22(16)20)24(34)32-26-28-8-10-36-26/h1-14H,(H,27,31,33)(H,28,32,34)
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University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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
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))		BDBM50264424
PNG
(CHEMBL4078891)
Show SMILES NC(=O)c1cnc2c(SSc3cccc4cc(cnc34)C(N)=O)cccc2c1
Show InChI InChI=1S/C20H14N4O2S2/c21-19(25)13-7-11-3-1-5-15(17(11)23-9-13)27-28-16-6-2-4-12-8-14(20(22)26)10-24-18(12)16/h1-10H,(H2,21,25)(H2,22,26)
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n/an/a 1.53E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264483
PNG
(CHEMBL4105598)
Show SMILES O=C(NCc1cccs1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3cccs3)cccc2c1
Show InChI InChI=1S/C30H22N4O2S4/c35-29(33-17-23-7-3-11-37-23)21-13-19-5-1-9-25(27(19)31-15-21)39-40-26-10-2-6-20-14-22(16-32-28(20)26)30(36)34-18-24-8-4-12-38-24/h1-16H,17-18H2,(H,33,35)(H,34,36)
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n/an/a 1.60E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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
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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n/an/a 1.80E+4n/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))		BDBM50264457
PNG
(CHEMBL4080490)
Show SMILES Fc1ccc(CNC(=O)c2cnc3c(SSc4cccc5cc(cnc45)C(=O)NCc4ccc(F)cc4)cccc3c2)cc1
Show InChI InChI=1S/C34H24F2N4O2S2/c35-27-11-7-21(8-12-27)17-39-33(41)25-15-23-3-1-5-29(31(23)37-19-25)43-44-30-6-2-4-24-16-26(20-38-32(24)30)34(42)40-18-22-9-13-28(36)14-10-22/h1-16,19-20H,17-18H2,(H,39,41)(H,40,42)
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n/an/a 1.80E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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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))		BDBM50264515
PNG
(CHEMBL4070821)
Show SMILES O=C(Nc1nccs1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)Nc3nccs3)cccc2c1
Show InChI InChI=1S/C26H16N6O2S4/c33-23(31-25-27-7-9-35-25)17-11-15-3-1-5-19(21(15)29-13-17)37-38-20-6-2-4-16-12-18(14-30-22(16)20)24(34)32-26-28-8-10-36-26/h1-14H,(H,27,31,33)(H,28,32,34)
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n/an/a 2.00E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264471
PNG
(CHEMBL4093962)
Show SMILES O=C(NCc1nccs1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCc3nccs3)cccc2c1
Show InChI InChI=1S/C28H20N6O2S4/c35-27(33-15-23-29-7-9-37-23)19-11-17-3-1-5-21(25(17)31-13-19)39-40-22-6-2-4-18-12-20(14-32-26(18)22)28(36)34-16-24-30-8-10-38-24/h1-14H,15-16H2,(H,33,35)(H,34,36)
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n/an/a 2.40E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264490
PNG
(CHEMBL4063134)
Show SMILES Cc1ccnc2c(S)cccc12
Show InChI InChI=1S/C10H9NS/c1-7-5-6-11-10-8(7)3-2-4-9(10)12/h2-6,12H,1H3
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n/an/a 2.51E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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n/an/a 3.00E+4n/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))		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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n/an/a 3.00E+4n/an/an/an/a7.5n/a



California Institute of Technology



Assay Description
Csn5 activity was measured using purified CSN complex and the fluorescent substrate OGNedd8–SCFSkp2, in which a unique cysteine engineered into ...

Nat Chem Biol 13: 486-493 (2017)


Article DOI: 10.1038/nchembio.2326
BindingDB Entry DOI: 10.7270/Q24J0D0B
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264419
PNG
(CHEMBL4073553)
Show SMILES O=C(NCCc1nccs1)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCCc3nccs3)cccc2c1
Show InChI InChI=1S/C30H24N6O2S4/c37-29(33-9-7-25-31-11-13-39-25)21-15-19-3-1-5-23(27(19)35-17-21)41-42-24-6-2-4-20-16-22(18-36-28(20)24)30(38)34-10-8-26-32-12-14-40-26/h1-6,11-18H,7-10H2,(H,33,37)(H,34,38)
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n/an/a 3.00E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
More data for this
Ligand-Target Pair
COP9 signalosome complex subunit 5


(Homo sapiens (Human))		BDBM50264451
PNG
(CHEMBL4080694)
Show SMILES O=C(CNC(=O)c1cnc2c(SSc3cccc4cc(cnc34)C(=O)NCC(=O)NCC(=O)OCc3ccccc3)cccc2c1)NCC(=O)OCc1ccccc1
Show InChI InChI=1S/C42H36N6O8S2/c49-35(43-23-37(51)55-25-27-9-3-1-4-10-27)21-47-41(53)31-17-29-13-7-15-33(39(29)45-19-31)57-58-34-16-8-14-30-18-32(20-46-40(30)34)42(54)48-22-36(50)44-24-38(52)56-26-28-11-5-2-6-12-28/h1-20H,21-26H2,(H,43,49)(H,44,50)(H,47,53)(H,48,54)
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n/an/a>3.00E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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n/an/a 3.20E+4n/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))		BDBM50264500
PNG
(CHEMBL4103114)
Show SMILES O=C(NCCc1nccs1)c1ccc2c(SSc3cccc4nc(ccc34)C(=O)NCCc3nccs3)cccc2n1
Show InChI InChI=1S/C30H24N6O2S4/c37-29(33-13-11-27-31-15-17-39-27)23-9-7-19-21(35-23)3-1-5-25(19)41-42-26-6-2-4-22-20(26)8-10-24(36-22)30(38)34-14-12-28-32-16-18-40-28/h1-10,15-18H,11-14H2,(H,33,37)(H,34,38)
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n/an/a 3.50E+4n/an/an/an/an/an/a



University of California San Diego

Curated by ChEMBL


Assay Description
Inhibition of CSN5 (unknown origin) using SCFskp2-Nedd8OG as substrate after 1 hr by fluorescence polarization assay

J Med Chem 60: 1343-1361 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01379
BindingDB Entry DOI: 10.7270/Q22F7QX5
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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n/an/a 3.50E+4n/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
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