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USPatent US10301317

Compile Data Set for Download or QSAR

Found 373 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
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM272554
PNG
(US10065967, Example 20 | US10301317, Example 2 | U...)
Show SMILES C[C@@H](N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1)c1ccccc1 |r|
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n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318077
PNG
(US10301317, Example 33 | US9624228, Example 33)
Show SMILES CN1CCC[C@H](C1)N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318080
PNG
(US10301317, Example 36 | US9624228, Example 36)
Show SMILES COc1ccc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc4ccc(F)c(Cl)c4)Cc3cc12
Show InChI InChI=1S/C22H17ClFN5O2/c1-31-20-5-3-13(9-25-20)21-15-7-14-11-29(10-12-2-4-17(24)16(23)6-12)22(30)26-18(14)8-19(15)27-28-21/h2-9H,10-11H2,1H3,(H,26,30)(H,27,28)
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n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318085
PNG
(US10301317, Example 41 | US9624228, Example 41)
Show SMILES Cn1cc(ccc1=O)-c1n[nH]c2cc3NC(=O)N(Cc4ccc(F)c(Cl)c4)Cc3cc12
Show InChI InChI=1S/C22H17ClFN5O2/c1-28-10-13(3-5-20(28)30)21-15-7-14-11-29(9-12-2-4-17(24)16(23)6-12)22(31)25-18(14)8-19(15)26-27-21/h2-8,10H,9,11H2,1H3,(H,25,31)(H,26,27)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318087
PNG
(US10301317, Example 43 | US9624228, Example 43)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(CCO)Cc3cc12
Show InChI InChI=1S/C17H17N5O2/c1-10-6-11(2-3-18-10)16-13-7-12-9-22(4-5-23)17(24)19-14(12)8-15(13)20-21-16/h2-3,6-8,23H,4-5,9H2,1H3,(H,19,24)(H,20,21)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318088
PNG
(US10301317, Example 44 | US9624228, Example 44)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)C1CCOCC1
Show InChI InChI=1S/C20H21N5O2/c1-12-8-13(2-5-21-12)19-16-9-14-11-25(15-3-6-27-7-4-15)20(26)22-17(14)10-18(16)23-24-19/h2,5,8-10,15H,3-4,6-7,11H2,1H3,(H,22,26)(H,23,24)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318089
PNG
(US10301317, Example 45 | US9624228, Example 45)
Show SMILES COCCOCCN1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1
Show InChI InChI=1S/C20H23N5O3/c1-13-9-14(3-4-21-13)19-16-10-15-12-25(5-6-28-8-7-27-2)20(26)22-17(15)11-18(16)23-24-19/h3-4,9-11H,5-8,12H2,1-2H3,(H,22,26)(H,23,24)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318093
PNG
(US10301317, Example 49 | US9624228, Example 49)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCOC1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318098
PNG
(US10301317, Example 54 | US9624228, Example 54)
Show SMILES C[C@H](CO)N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318114
PNG
(US10301317, Example 70 | US9624228, Example 70)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)C1CCN(Cc2ccccc2)CC1
Show InChI InChI=1S/C27H28N6O/c1-18-13-20(7-10-28-18)26-23-14-21-17-33(27(34)29-24(21)15-25(23)30-31-26)22-8-11-32(12-9-22)16-19-5-3-2-4-6-19/h2-7,10,13-15,22H,8-9,11-12,16-17H2,1H3,(H,29,34)(H,30,31)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318148
PNG
(US10301317, Example 104 | US9624228, Example 104)
Show SMILES COc1ncc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2ccccc2)C1 |r|
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n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318171
PNG
(US10301317, Example 127 | US9624228, Example 127)
Show SMILES Fc1cc(F)cc(CN2Cc3cc4c(n[nH]c4cc3NC2=O)-c2ccnnc2)c1
Show InChI InChI=1S/C20H14F2N6O/c21-14-3-11(4-15(22)6-14)9-28-10-13-5-16-18(7-17(13)25-20(28)29)26-27-19(16)12-1-2-23-24-8-12/h1-8H,9-10H2,(H,25,29)(H,26,27)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318172
PNG
(US10301317, Example 128 | US9624228, Example 128)
Show SMILES O=C1Nc2cc3[nH]nc(-c4ccnnc4)c3cc2CN1Cc1cccc(c1)C#N
Show InChI InChI=1S/C21H15N7O/c22-9-13-2-1-3-14(6-13)11-28-12-16-7-17-19(8-18(16)25-21(28)29)26-27-20(17)15-4-5-23-24-10-15/h1-8,10H,11-12H2,(H,25,29)(H,26,27)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318107
PNG
(US10301317, Example 165 | US9624228, Example 148 |...)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2ccccc2)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318200
PNG
(US10301317, Example 156 | US9624228, Example 156)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2cccc(Cl)c2)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318205
PNG
(US10301317, Example 161 | US9624228, Example 161)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2cccnc2C(F)(F)F)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318107
PNG
(US10301317, Example 165 | US9624228, Example 148 |...)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2ccccc2)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318218
PNG
(US10301317, Example 174 | US9624228, Example 174)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(C1)c1cccc(Cl)c1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318231
PNG
(US10301317, Example 187 | US9624228, Example 187)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2cc(F)ccc2F)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318237
PNG
(US10301317, Example 193 | US9624228, Example 193)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(CC(F)(F)F)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM393184
PNG
(US10301317, Example 197)
Show SMILES CC(N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1)c1ccc(F)cc1
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318249
PNG
(US10301317, Example 205 | US9624228, Example 205)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)C1CCCC1
Show InChI InChI=1S/C20H21N5O/c1-12-8-13(6-7-21-12)19-16-9-14-11-25(15-4-2-3-5-15)20(26)22-17(14)10-18(16)23-24-19/h6-10,15H,2-5,11H2,1H3,(H,22,26)(H,23,24)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318261
PNG
(US10301317, Example 217 | US9624228, Example 217)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc4ccccc4Cl)Cc3cc12
Show InChI InChI=1S/C22H18ClN5O/c1-13-8-14(6-7-24-13)21-17-9-16-12-28(11-15-4-2-3-5-18(15)23)22(29)25-19(16)10-20(17)26-27-21/h2-10H,11-12H2,1H3,(H,25,29)(H,26,27)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318263
PNG
(US10301317, Example 219 | US9624228, Example 219)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)C1CCOC(C)(C)C1
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318287
PNG
(US10301317, Example 244 | US9624228, Example 244)
Show SMILES Cc1cc(cc(C)n1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(CC(F)(F)F)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318288
PNG
(US10301317, Example 245 | US9624228, Example 245)
Show SMILES Cc1ccc(CN2CCC[C@H](C2)N2Cc3cc4c(n[nH]c4cc3NC2=O)-c2ccnc(C)c2)s1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318302
PNG
(US10301317, Example 259 | US9624228, Example 259)
Show SMILES Cn1cc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCN(CC(F)(F)F)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318332
PNG
(US10301317, Example 289 | US9624228, Example 289)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3[nH]c(=O)c(cc3cc12)C1CCCC1
Show InChI InChI=1S/C21H20N4O/c1-12-8-14(6-7-22-12)20-17-10-15-9-16(13-4-2-3-5-13)21(26)23-18(15)11-19(17)24-25-20/h6-11,13H,2-5H2,1H3,(H,23,26)(H,24,25)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318322
PNG
(US10301317, Example 297 | US9624228, Example 279 |...)
Show SMILES CC(C)N1C[C@H]([C@@H](C1)c1ccccc1)N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318389
PNG
(US10301317, Example 347 | US9624228, Example 347)
Show SMILES CC(c1ccccc1)c1cc2cc3c(n[nH]c3cc2[nH]c1=O)-c1ccc(=O)n(C)c1
Show InChI InChI=1S/C24H18N4O2/c1-14(15-6-4-3-5-7-15)18-10-17-11-19-21(12-20(17)25-24(18)30)26-27-23(19)16-8-9-22(29)28(2)13-16/h3-14H,1-2H3
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318390
PNG
(US10301317, Example 348 | US9624228, Example 348)
Show SMILES COc1ncc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CN(CC(F)(F)F)C[C@H]1c1ccccc1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318418
PNG
(US10301317, Example 376 | US9624228, Example 376)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CN(CCO)C[C@H]1c1ccccc1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318053
PNG
(US10301317, Example 9 | US9624228, Example 9)
Show SMILES COc1ncccc1CN1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1
Show InChI InChI=1S/C22H20N6O2/c1-13-8-14(5-7-23-13)20-17-9-16-12-28(11-15-4-3-6-24-21(15)30-2)22(29)25-18(16)10-19(17)26-27-20/h3-10H,11-12H2,1-2H3,(H,25,29)(H,26,27)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318054
PNG
(US10301317, Example 10 | US9624228, Example 10)
Show SMILES COc1ccc(CN2Cc3cc4c(n[nH]c4cc3NC2=O)-c2ccnc(C)c2)cc1
Show InChI InChI=1S/C23H21N5O2/c1-14-9-16(7-8-24-14)22-19-10-17-13-28(12-15-3-5-18(30-2)6-4-15)23(29)25-20(17)11-21(19)26-27-22/h3-11H,12-13H2,1-2H3,(H,25,29)(H,26,27)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318062
PNG
(US10301317, Example 18 | US9624228, Example 18)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(CCc4ccc(F)cc4)Cc3cc12
Show InChI InChI=1S/C23H20FN5O/c1-14-10-16(6-8-25-14)22-19-11-17-13-29(9-7-15-2-4-18(24)5-3-15)23(30)26-20(17)12-21(19)27-28-22/h2-6,8,10-12H,7,9,13H2,1H3,(H,26,30)(H,27,28)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318066
PNG
(US10301317, Example 22 | US9624228, Example 22)
Show SMILES CC(c1ccccc1)c1cc2cc3c(n[nH]c3cc2[nH]c1=O)-c1ccnc(C)c1
Show InChI InChI=1S/C24H18N4O/c1-14-10-17(8-9-25-14)23-20-12-18-11-19(15(2)16-6-4-3-5-7-16)24(29)26-21(18)13-22(20)27-28-23/h3-13,15H,1-2H3
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318075
PNG
(US10301317, Example 31 | US9624228, Example 31)
Show SMILES Cn1cc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc4ccc(F)c(Cl)c4)Cc3cc12
Show InChI InChI=1S/C20H16ClFN6O/c1-27-9-13(7-23-27)19-14-5-12-10-28(8-11-2-3-16(22)15(21)4-11)20(29)24-17(12)6-18(14)25-26-19/h2-7,9H,8,10H2,1H3,(H,24,29)(H,25,26)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318097
PNG
(US10301317, Example 53 | US9624228, Example 53)
Show SMILES CC(C)CC(C)N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnc(C)c1
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318105
PNG
(US10301317, Example 61 | US9624228, Example 61)
Show SMILES Clc1cccc(CN2Cc3cc4c(n[nH]c4cc3NC2=O)-c2ccc(=O)[nH]c2)c1
Show InChI InChI=1S/C21H16ClN5O2/c22-15-3-1-2-12(6-15)10-27-11-14-7-16-18(8-17(14)24-21(27)29)25-26-20(16)13-4-5-19(28)23-9-13/h1-9H,10-11H2,(H,23,28)(H,24,29)(H,25,26)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318107
PNG
(US10301317, Example 165 | US9624228, Example 148 |...)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2ccccc2)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318123
PNG
(US10301317, Example 79 | US9624228, Example 79)
Show SMILES COc1ccc(cn1)-c1n[nH]c2cc3NC(=O)N(CCc4ccc(F)cc4)Cc3cc12
Show InChI InChI=1S/C23H20FN5O2/c1-31-21-7-4-15(12-25-21)22-18-10-16-13-29(9-8-14-2-5-17(24)6-3-14)23(30)26-19(16)11-20(18)27-28-22/h2-7,10-12H,8-9,13H2,1H3,(H,26,30)(H,27,28)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318124
PNG
(US10301317, Example 80 | US9624228, Example 80)
Show SMILES COc1ncc(cn1)-c1n[nH]c2cc3NC(=O)N(CCc4ccc(F)cc4)Cc3cc12
Show InChI InChI=1S/C22H19FN6O2/c1-31-21-24-10-15(11-25-21)20-17-8-14-12-29(7-6-13-2-4-16(23)5-3-13)22(30)26-18(14)9-19(17)27-28-20/h2-5,8-11H,6-7,12H2,1H3,(H,26,30)(H,27,28)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318129
PNG
(US10301317, Example 85 | US9624228, Example 85)
Show SMILES COc1ccc(cn1)-c1n[nH]c2cc3NC(=O)N(CCc4cccc(Cl)c4)Cc3cc12
Show InChI InChI=1S/C23H20ClN5O2/c1-31-21-6-5-15(12-25-21)22-18-10-16-13-29(8-7-14-3-2-4-17(24)9-14)23(30)26-19(16)11-20(18)27-28-22/h2-6,9-12H,7-8,13H2,1H3,(H,26,30)(H,27,28)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318143
PNG
(US10301317, Example 99 | US9624228, Example 99)
Show SMILES COc1ncc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc4ccc(F)cc4F)Cc3cc12
Show InChI InChI=1S/C21H16F2N6O2/c1-31-20-24-7-13(8-25-20)19-15-4-12-10-29(9-11-2-3-14(22)5-16(11)23)21(30)26-17(12)6-18(15)27-28-19/h2-8H,9-10H2,1H3,(H,26,30)(H,27,28)
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318146
PNG
(US10301317, Example 102 | US9624228, Example 102)
Show SMILES COc1ncc(cn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2c(F)cccc2F)C1 |r|
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GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318155
PNG
(US10301317, Example 111 | US9624228, Example 111)
Show SMILES C[C@@H](N1Cc2cc3c(n[nH]c3cc2NC1=O)-c1ccnnc1)c1cccc(Cl)c1 |r|
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UniChem
US Patent
n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318187
PNG
(US10301317, Example 143 | US9624228, Example 143)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2c(F)cccc2F)C1 |r|
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PC cid
PC sid
UniChem
US Patent
n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318189
PNG
(US10301317, Example 145 | US9624228, Example 145)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(CCc2ccccc2)C1 |r|
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n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318195
PNG
(US10301317, Example 151 | US9624228, Example 151)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2ccc(F)cc2)C1 |r|
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UniChem
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n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
Mitogen-activated protein kinase 1


(Homo sapiens (Human))		BDBM318210
PNG
(US10301317, Example 166 | US9624228, Example 166)
Show SMILES Cc1cc(ccn1)-c1n[nH]c2cc3NC(=O)N(Cc3cc12)[C@@H]1CCCN(Cc2cncnc2)C1 |r|
PDB
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PC cid
PC sid
UniChem
US Patent
n/an/a<50n/an/an/an/an/an/a



GSK



Assay Description
The inhibition of ERK activity by the compounds disclosed herein was determined using the Z′-LYTE kinase assay kit (Life Technologies) with a S...

Bioorg Med Chem Lett 18: 5018-22 (2008)


BindingDB Entry DOI: 10.7270/Q2GM89M0
More data for this
Ligand-Target Pair
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* indicates data uncertainty>20%