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Found 192 hits of Enz. Inhib. data with enzyme = 'Epidermal growth factor receptor' and Substrate = 'EGF-R Tyrosine Kinase'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5140
PNG
(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-oxo-...)
Show SMILES CCN(CC)CC(O)CNC(=O)c1cc(C)c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)[nH]1
Show InChI InChI=1S/C26H29ClFN7O3/c1-4-35(5-2)12-16(36)11-29-26(38)21-8-14(3)20(33-21)10-17-22-23(30-13-31-24(22)34-25(17)37)32-15-6-7-19(28)18(27)9-15/h6-10,13,16,33,36H,4-5,11-12H2,1-3H3,(H,29,38)(H2,30,31,32,34,37)/b17-10-
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n/an/a 0.450n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5146
PNG
(5-{[(5Z)-4-[(1-benzyl-1H-indol-5-yl)amino]-6-oxo-5...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc4n(Cc5ccccc5)ccc4c3)c12)C(=O)NCCN1CCOCC1
Show InChI InChI=1S/C34H34N8O3/c1-22-17-28(34(44)35-10-12-41-13-15-45-16-14-41)39-27(22)19-26-30-31(36-21-37-32(30)40-33(26)43)38-25-7-8-29-24(18-25)9-11-42(29)20-23-5-3-2-4-6-23/h2-9,11,17-19,21,39H,10,12-16,20H2,1H3,(H,35,44)(H2,36,37,38,40,43)/b26-19-
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n/an/a 1.10n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5138
PNG
(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-oxo-...)
Show SMILES CCN(CC)CCNC(=O)c1cc(C)c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)[nH]1
Show InChI InChI=1S/C25H27ClFN7O2/c1-4-34(5-2)9-8-28-25(36)20-10-14(3)19(32-20)12-16-21-22(29-13-30-23(21)33-24(16)35)31-15-6-7-18(27)17(26)11-15/h6-7,10-13,32H,4-5,8-9H2,1-3H3,(H,28,36)(H2,29,30,31,33,35)/b16-12-
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n/an/a 1.20n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5145
PNG
((5Z)-4-[(1-benzyl-1H-indazol-5-yl)amino]-5-{[3-met...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc4n(Cc5ccccc5)ncc4c3)c12)C(=O)N1CCOCC1
Show InChI InChI=1S/C31H28N8O3/c1-19-13-25(31(41)38-9-11-42-12-10-38)36-24(19)15-23-27-28(32-18-33-29(27)37-30(23)40)35-22-7-8-26-21(14-22)16-34-39(26)17-20-5-3-2-4-6-20/h2-8,13-16,18,36H,9-12,17H2,1H3,(H2,32,33,35,37,40)/b23-15-
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n/an/a 1.80n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4567
PNG
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)C=C)cc23)c1
Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22)
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n/an/a 2n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4582
PNG
(4-anilinoquinazoline deriv. 10o | N-{4-[(3-bromoph...)
Show SMILES OCC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C18H13BrN4O2/c19-12-3-1-4-13(9-12)23-18-15-10-14(22-17(25)5-2-8-24)6-7-16(15)20-11-21-18/h1,3-4,6-7,9-11,24H,8H2,(H,22,25)(H,20,21,23)
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n/an/a 2n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5134
PNG
((5Z)-4-[(3-chloro-4-fluorophenyl)amino]-5-({3-meth...)
Show SMILES CN1CCN(CC1)C(=O)c1cc(C)c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)[nH]1
Show InChI InChI=1S/C24H23ClFN7O2/c1-13-9-19(24(35)33-7-5-32(2)6-8-33)30-18(13)11-15-20-21(27-12-28-22(20)31-23(15)34)29-14-3-4-17(26)16(25)10-14/h3-4,9-12,30H,5-8H2,1-2H3,(H2,27,28,29,31,34)/b15-11-
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n/an/a 2.80n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5144
PNG
((5Z)-4-[(1-benzyl-1H-indol-5-yl)amino]-5-{[3-methy...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc4n(Cc5ccccc5)ccc4c3)c12)C(=O)N1CCOCC1
Show InChI InChI=1S/C32H29N7O3/c1-20-15-26(32(41)38-11-13-42-14-12-38)36-25(20)17-24-28-29(33-19-34-30(28)37-31(24)40)35-23-7-8-27-22(16-23)9-10-39(27)18-21-5-3-2-4-6-21/h2-10,15-17,19,36H,11-14,18H2,1H3,(H2,33,34,35,37,40)/b24-17-
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n/an/a 4.5n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5127
PNG
(3-(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-o...)
Show SMILES Cc1cc(CCC(O)=O)[nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc(F)c(Cl)c3)c12
Show InChI InChI=1S/C21H17ClFN5O3/c1-10-6-11(3-5-17(29)30)26-16(10)8-13-18-19(24-9-25-20(18)28-21(13)31)27-12-2-4-15(23)14(22)7-12/h2,4,6-9,26H,3,5H2,1H3,(H,29,30)(H2,24,25,27,28,31)/b13-8-
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n/an/a 4.70n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5139
PNG
((5Z)-4-[(3-chloro-4-fluorophenyl)amino]-5-({5-[(3,...)
Show SMILES CC1CN(CC(C)N1)C(=O)c1cc(C)c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)[nH]1
Show InChI InChI=1S/C25H25ClFN7O2/c1-12-6-20(25(36)34-9-13(2)30-14(3)10-34)32-19(12)8-16-21-22(28-11-29-23(21)33-24(16)35)31-15-4-5-18(27)17(26)7-15/h4-8,11,13-14,30,32H,9-10H2,1-3H3,(H2,28,29,31,33,35)/b16-8-
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n/an/a 5.90n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4568
PNG
(4-anilinoquinazoline deriv. 10a | N-{4-[(3-bromoph...)
Show SMILES CN(C)CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C20H18BrN5O/c1-26(2)10-4-7-19(27)24-16-8-9-18-17(12-16)20(23-13-22-18)25-15-6-3-5-14(21)11-15/h3,5-6,8-9,11-13H,10H2,1-2H3,(H,24,27)(H,22,23,25)
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n/an/a 6n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5130
PNG
(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-oxo-...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc(F)c(Cl)c3)c12)C(=O)NCCN1CCOCC1
Show InChI InChI=1S/C25H25ClFN7O3/c1-14-10-20(25(36)28-4-5-34-6-8-37-9-7-34)32-19(14)12-16-21-22(29-13-30-23(21)33-24(16)35)31-15-2-3-18(27)17(26)11-15/h2-3,10-13,32H,4-9H2,1H3,(H,28,36)(H2,29,30,31,33,35)/b16-12-
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n/an/a 6.5n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4566
PNG
(4-anilinoquinazoline deriv. 1 | CHEMBL91867 | N-{4...)
Show SMILES CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
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n/an/a 8n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4579
PNG
(4-anilinoquinazoline deriv. 10l | N-{4-[(3-bromoph...)
Show SMILES COCC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C19H15BrN4O2/c1-26-9-3-6-18(25)23-15-7-8-17-16(11-15)19(22-12-21-17)24-14-5-2-4-13(20)10-14/h2,4-5,7-8,10-12H,9H2,1H3,(H,23,25)(H,21,22,24)
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n/an/a 9n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4583
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES CN(C)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C20H20BrN5O/c1-26(2)10-4-7-19(27)24-16-8-9-18-17(12-16)20(23-13-22-18)25-15-6-3-5-14(21)11-15/h3-9,11-13H,10H2,1-2H3,(H,24,27)(H,22,23,25)/b7-4+
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n/an/a 11n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4569
PNG
(4-anilinoquinazoline deriv. 10b | N-{4-[(3-bromoph...)
Show SMILES CCN(CC)CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C22H22BrN5O/c1-3-28(4-2)12-6-9-21(29)26-18-10-11-20-19(14-18)22(25-15-24-20)27-17-8-5-7-16(23)13-17/h5,7-8,10-11,13-15H,3-4,12H2,1-2H3,(H,26,29)(H,24,25,27)
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n/an/a 12n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5137
PNG
((5Z)-4-[(3-chloro-4-fluorophenyl)amino]-5-({5-[(4-...)
Show SMILES CCN1CCN(CC1)C(=O)c1cc(C)c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)[nH]1
Show InChI InChI=1S/C25H25ClFN7O2/c1-3-33-6-8-34(9-7-33)25(36)20-10-14(2)19(31-20)12-16-21-22(28-13-29-23(21)32-24(16)35)30-15-4-5-18(27)17(26)11-15/h4-5,10-13,31H,3,6-9H2,1-2H3,(H2,28,29,30,32,35)/b16-12-
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n/an/a 13n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4592
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES CN(CCO)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C21H22BrN5O2/c1-27(10-11-28)9-3-6-20(29)25-17-7-8-19-18(13-17)21(24-14-23-19)26-16-5-2-4-15(22)12-16/h2-8,12-14,28H,9-11H2,1H3,(H,25,29)(H,23,24,26)/b6-3+
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n/an/a 14n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5141
PNG
(5-{[(5Z)-4-[(3-ethynylphenyl)amino]-6-oxo-5H,6H,7H...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3cccc(c3)C#C)c12)C(=O)NCCN1CCOCC1
Show InChI InChI=1S/C27H27N7O3/c1-3-18-5-4-6-19(14-18)31-24-23-20(26(35)33-25(23)30-16-29-24)15-21-17(2)13-22(32-21)27(36)28-7-8-34-9-11-37-12-10-34/h1,4-6,13-16,32H,7-12H2,2H3,(H,28,36)(H2,29,30,31,33,35)/b20-15-
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n/an/a 18n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4575
PNG
(4-anilinoquinazoline deriv. 10h | N-{4-[(3-bromoph...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)C#CCN4CCOCC4)cc23)c1
Show InChI InChI=1S/C22H20BrN5O2/c23-16-3-1-4-17(13-16)27-22-19-14-18(6-7-20(19)24-15-25-22)26-21(29)5-2-8-28-9-11-30-12-10-28/h1,3-4,6-7,13-15H,8-12H2,(H,26,29)(H,24,25,27)
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n/an/a 20n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5129
PNG
(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-oxo-...)
Show SMILES Fc1ccc(Nc2ncnc3NC(=O)\C(=C/c4ccc([nH]4)C(=O)NCCN4CCOCC4)c23)cc1Cl
Show InChI InChI=1S/C24H23ClFN7O3/c25-17-12-15(1-3-18(17)26)31-21-20-16(23(34)32-22(20)29-13-28-21)11-14-2-4-19(30-14)24(35)27-5-6-33-7-9-36-10-8-33/h1-4,11-13,30H,5-10H2,(H,27,35)(H2,28,29,31,32,34)/b16-11-
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n/an/a 22n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5128
PNG
(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-oxo-...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc(F)c(Cl)c3)c12)C(O)=O
Show InChI InChI=1S/C19H13ClFN5O3/c1-8-4-14(19(28)29)25-13(8)6-10-15-16(22-7-23-17(15)26-18(10)27)24-9-2-3-12(21)11(20)5-9/h2-7,25H,1H3,(H,28,29)(H2,22,23,24,26,27)/b10-6-
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n/an/a 29n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5126
PNG
((5Z)-4-[(3-chloro-4-fluorophenyl)amino]-5-[(3,5-di...)
Show SMILES Cc1cc(C)c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)[nH]1
Show InChI InChI=1S/C19H15ClFN5O/c1-9-5-10(2)24-15(9)7-12-16-17(22-8-23-18(16)26-19(12)27)25-11-3-4-14(21)13(20)6-11/h3-8,24H,1-2H3,(H2,22,23,25,26,27)/b12-7-
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n/an/a 41n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4574
PNG
(4-anilinoquinazoline deriv. 10g | N-{4-[(3-bromoph...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)C#CCN4CCCCC4)cc23)c1
Show InChI InChI=1S/C23H22BrN5O/c24-17-6-4-7-18(14-17)28-23-20-15-19(9-10-21(20)25-16-26-23)27-22(30)8-5-13-29-11-2-1-3-12-29/h4,6-7,9-10,14-16H,1-3,11-13H2,(H,27,30)(H,25,26,28)
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n/an/a 57n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4581
PNG
(4-anilinoquinazoline deriv. 10n | CHEMBL93049 | N-...)
Show SMILES COCOCC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C20H17BrN4O3/c1-27-13-28-9-3-6-19(26)24-16-7-8-18-17(11-16)20(23-12-22-18)25-15-5-2-4-14(21)10-15/h2,4-5,7-8,10-12H,9,13H2,1H3,(H,24,26)(H,22,23,25)
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n/an/a 59n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4591
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES COCCN(C)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C22H24BrN5O2/c1-28(11-12-30-2)10-4-7-21(29)26-18-8-9-20-19(14-18)22(25-15-24-20)27-17-6-3-5-16(23)13-17/h3-9,13-15H,10-12H2,1-2H3,(H,26,29)(H,24,25,27)/b7-4+
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n/an/a 62n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4570
PNG
(4-anilinoquinazoline deriv. 10c | N-{4-[(3-bromoph...)
Show SMILES CCCN(CCC)CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C24H26BrN5O/c1-3-12-30(13-4-2)14-6-9-23(31)28-20-10-11-22-21(16-20)24(27-17-26-22)29-19-8-5-7-18(25)15-19/h5,7-8,10-11,15-17H,3-4,12-14H2,1-2H3,(H,28,31)(H,26,27,29)
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n/an/a 62n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4580
PNG
(4-anilinoquinazoline deriv. 10m | N-{4-[(3-bromoph...)
Show SMILES COCCOCC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C21H19BrN4O3/c1-28-10-11-29-9-3-6-20(27)25-17-7-8-19-18(13-17)21(24-14-23-19)26-16-5-2-4-15(22)12-16/h2,4-5,7-8,12-14H,9-11H2,1H3,(H,25,27)(H,23,24,26)
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n/an/a 65n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4578
PNG
(4-anilinoquinazoline deriv. 10k | N-{4-[(3-bromoph...)
Show SMILES CCN1CCN(CC#CC(=O)Nc2ccc3ncnc(Nc4cccc(Br)c4)c3c2)CC1
Show InChI InChI=1S/C24H25BrN6O/c1-2-30-11-13-31(14-12-30)10-4-7-23(32)28-20-8-9-22-21(16-20)24(27-17-26-22)29-19-6-3-5-18(25)15-19/h3,5-6,8-9,15-17H,2,10-14H2,1H3,(H,28,32)(H,26,27,29)
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n/an/a 65n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4577
PNG
(4-anilinoquinazoline deriv. 10j | N-{4-[(3-bromoph...)
Show SMILES COC[C@@H]1CCCN1CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C24H24BrN5O2/c1-32-15-20-7-3-11-30(20)12-4-8-23(31)28-19-9-10-22-21(14-19)24(27-16-26-22)29-18-6-2-5-17(25)13-18/h2,5-6,9-10,13-14,16,20H,3,7,11-12,15H2,1H3,(H,28,31)(H,26,27,29)/t20-/m0/s1
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n/an/a 65n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4593
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)\C=C\CN4CCC(CC4)N4CCCCC4)cc23)c1
Show InChI InChI=1S/C28H33BrN6O/c29-21-6-4-7-22(18-21)33-28-25-19-23(9-10-26(25)30-20-31-28)32-27(36)8-5-13-34-16-11-24(12-17-34)35-14-2-1-3-15-35/h4-10,18-20,24H,1-3,11-17H2,(H,32,36)(H,30,31,33)/b8-5+
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n/an/a 68n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM3032
PNG
(CHEMBL1204168 | CHEMBL29197 | N-(3-bromophenyl)-6,...)
Show SMILES COc1cc2ncnc(Nc3cccc(Br)c3)c2cc1OC
Show InChI InChI=1S/C16H14BrN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
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n/an/a 70n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 43: 3244-56 (2000)


Article DOI: 10.1021/jm000206a
BindingDB Entry DOI: 10.7270/Q22V2D9M
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4573
PNG
(4-anilinoquinazoline deriv. 10f | N-{4-[(3-bromoph...)
Show SMILES CN(CC=C)CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C22H20BrN5O/c1-3-11-28(2)12-5-8-21(29)26-18-9-10-20-19(14-18)22(25-15-24-20)27-17-7-4-6-16(23)13-17/h3-4,6-7,9-10,13-15H,1,11-12H2,2H3,(H,26,29)(H,24,25,27)
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n/an/a 71n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4584
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES CCN(CC)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C22H24BrN5O/c1-3-28(4-2)12-6-9-21(29)26-18-10-11-20-19(14-18)22(25-15-24-20)27-17-8-5-7-16(23)13-17/h5-11,13-15H,3-4,12H2,1-2H3,(H,26,29)(H,24,25,27)/b9-6+
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n/an/a 73n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4587
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)\C=C\CN4CCOCC4)cc23)c1
Show InChI InChI=1S/C22H22BrN5O2/c23-16-3-1-4-17(13-16)27-22-19-14-18(6-7-20(19)24-15-25-22)26-21(29)5-2-8-28-9-11-30-12-10-28/h1-7,13-15H,8-12H2,(H,26,29)(H,24,25,27)/b5-2+
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n/an/a 74n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4590
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES COC[C@H]1CCCN1C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C24H26BrN5O2/c1-32-15-20-7-3-11-30(20)12-4-8-23(31)28-19-9-10-22-21(14-19)24(27-16-26-22)29-18-6-2-5-17(25)13-18/h2,4-6,8-10,13-14,16,20H,3,7,11-12,15H2,1H3,(H,28,31)(H,26,27,29)/b8-4+/t20-/m1/s1
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n/an/a 85n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4571
PNG
(4-anilinoquinazoline deriv. 10d | N-{4-[(3-bromoph...)
Show SMILES CC(C)N(C)CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C22H22BrN5O/c1-15(2)28(3)11-5-8-21(29)26-18-9-10-20-19(13-18)22(25-14-24-20)27-17-7-4-6-16(23)12-17/h4,6-7,9-10,12-15H,11H2,1-3H3,(H,26,29)(H,24,25,27)
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n/an/a 85n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4585
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES CCCN(CCC)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C24H28BrN5O/c1-3-12-30(13-4-2)14-6-9-23(31)28-20-10-11-22-21(16-20)24(27-17-26-22)29-19-8-5-7-18(25)15-19/h5-11,15-17H,3-4,12-14H2,1-2H3,(H,28,31)(H,26,27,29)/b9-6+
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n/an/a 90n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4576
PNG
(4-anilinoquinazoline deriv. 10i | N-{4-[(3-bromoph...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)C#CCN4CCSCC4)cc23)c1
Show InChI InChI=1S/C22H20BrN5OS/c23-16-3-1-4-17(13-16)27-22-19-14-18(6-7-20(19)24-15-25-22)26-21(29)5-2-8-28-9-11-30-12-10-28/h1,3-4,6-7,13-15H,8-12H2,(H,26,29)(H,24,25,27)
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n/an/a 95n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4572
PNG
(4-[bis(propan-2-yl)amino]-N-{4-[(3-bromophenyl)ami...)
Show SMILES CC(C)N(CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1)C(C)C
Show InChI InChI=1S/C24H26BrN5O/c1-16(2)30(17(3)4)12-6-9-23(31)28-20-10-11-22-21(14-20)24(27-15-26-22)29-19-8-5-7-18(25)13-19/h5,7-8,10-11,13-17H,12H2,1-4H3,(H,28,31)(H,26,27,29)
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n/an/a 97n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4586
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)\C=C\CN4CCCCC4)cc23)c1
Show InChI InChI=1S/C23H24BrN5O/c24-17-6-4-7-18(14-17)28-23-20-15-19(9-10-21(20)25-16-26-23)27-22(30)8-5-13-29-11-2-1-3-12-29/h4-10,14-16H,1-3,11-13H2,(H,27,30)(H,25,26,28)/b8-5+
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n/an/a 106n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4599
PNG
(4-anilinoquinazoline deriv. 23 | N-{4-[(3-bromophe...)
Show SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)C(=C)CN4CCOCC4)cc23)c1
Show InChI InChI=1S/C22H22BrN5O2/c1-15(13-28-7-9-30-10-8-28)22(29)27-18-5-6-20-19(12-18)21(25-14-24-20)26-17-4-2-3-16(23)11-17/h2-6,11-12,14H,1,7-10,13H2,(H,27,29)(H,24,25,26)
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n/an/a 107n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4598
PNG
(4-anilinoquinazoline deriv. 20 | N-{4-[(3-bromophe...)
Show SMILES CN1CCC=C(C1)C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C21H20BrN5O/c1-27-9-3-4-14(12-27)21(28)26-17-7-8-19-18(11-17)20(24-13-23-19)25-16-6-2-5-15(22)10-16/h2,4-8,10-11,13H,3,9,12H2,1H3,(H,26,28)(H,23,24,25)
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n/an/a 115n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4589
PNG
((2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES COC[C@@H]1CCCN1C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C24H26BrN5O2/c1-32-15-20-7-3-11-30(20)12-4-8-23(31)28-19-9-10-22-21(14-19)24(27-16-26-22)29-18-6-2-5-17(25)13-18/h2,4-6,8-10,13-14,16,20H,3,7,11-12,15H2,1H3,(H,28,31)(H,26,27,29)/b8-4+/t20-/m0/s1
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n/an/a 131n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4473
PNG
(4-(4-Fluoro-3-trifluoromethylphenylamino)-6,7-dime...)
Show SMILES COc1cc2ncc(C#N)c(Nc3ccc(F)c(c3)C(F)(F)F)c2cc1OC
Show InChI InChI=1S/C19H13F4N3O2/c1-27-16-6-12-15(7-17(16)28-2)25-9-10(8-24)18(12)26-11-3-4-14(20)13(5-11)19(21,22)23/h3-7,9H,1-2H3,(H,25,26)
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n/an/a 160n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 43: 3244-56 (2000)


Article DOI: 10.1021/jm000206a
BindingDB Entry DOI: 10.7270/Q22V2D9M
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5133
PNG
((5Z)-4-[(3-chloro-4-fluorophenyl)amino]-5-{[3-meth...)
Show SMILES Cc1cc([nH]c1\C=C1/C(=O)Nc2ncnc(Nc3ccc(F)c(Cl)c3)c12)C(=O)N1CCOCC1
Show InChI InChI=1S/C23H20ClFN6O3/c1-12-8-18(23(33)31-4-6-34-7-5-31)29-17(12)10-14-19-20(26-11-27-21(19)30-22(14)32)28-13-2-3-16(25)15(24)9-13/h2-3,8-11,29H,4-7H2,1H3,(H2,26,27,28,30,32)/b14-10-
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n/an/a 170n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4446
PNG
(4-(3-Chlorophenylamino)-6,7-dimethoxyquinoline-3-c...)
Show SMILES COc1cc2ncc(C#N)c(Nc3cccc(Cl)c3)c2cc1OC
Show InChI InChI=1S/C18H14ClN3O2/c1-23-16-7-14-15(8-17(16)24-2)21-10-11(9-20)18(14)22-13-5-3-4-12(19)6-13/h3-8,10H,1-2H3,(H,21,22)
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n/an/a 180n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 43: 3244-56 (2000)


Article DOI: 10.1021/jm000206a
BindingDB Entry DOI: 10.7270/Q22V2D9M
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM5124
PNG
(3-(5-{[(5Z)-4-[(3-chloro-4-fluorophenyl)amino]-6-o...)
Show SMILES Cc1[nH]c(\C=C2/C(=O)Nc3ncnc(Nc4ccc(F)c(Cl)c4)c23)c(C)c1CCC(O)=O
Show InChI InChI=1S/C22H19ClFN5O3/c1-10-13(4-6-18(30)31)11(2)27-17(10)8-14-19-20(25-9-26-21(19)29-22(14)32)28-12-3-5-16(24)15(23)7-12/h3,5,7-9,27H,4,6H2,1-2H3,(H,30,31)(H2,25,26,28,29,32)/b14-8-
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n/an/a 180n/an/an/an/an/an/a



SUGEN, Inc.



Assay Description
IC50 is the inhibitor concentration which inhibits 50% of EGF-R or PDGFR-beta kinase autophosphorylation activity. The assay was performed in 96-well...


Bioorg Med Chem Lett 12: 2153-7 (2002)


Article DOI: 10.1016/s0960-894x(02)00364-5
BindingDB Entry DOI: 10.7270/Q200009N
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4445
PNG
(4-(3-Bromophenylamino)-6,7-dimethoxyquinoline-3-ca...)
Show SMILES COc1cc2ncc(C#N)c(Nc3cccc(Br)c3)c2cc1OC
Show InChI InChI=1S/C18H14BrN3O2/c1-23-16-7-14-15(8-17(16)24-2)21-10-11(9-20)18(14)22-13-5-3-4-12(19)6-13/h3-8,10H,1-2H3,(H,21,22)
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n/an/a 190n/an/an/an/a7.422



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 43: 3244-56 (2000)


Article DOI: 10.1021/jm000206a
BindingDB Entry DOI: 10.7270/Q22V2D9M
More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (human))
BDBM4603
PNG
((2Z)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4...)
Show SMILES COC[C@@H]1CCCN1C\C=C/C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Show InChI InChI=1S/C24H26BrN5O2/c1-32-15-20-7-3-11-30(20)12-4-8-23(31)28-19-9-10-22-21(14-19)24(27-16-26-22)29-18-6-2-5-17(25)13-18/h2,4-6,8-10,13-14,16,20H,3,7,11-12,15H2,1H3,(H,28,31)(H,26,27,29)/b8-4-/t20-/m0/s1
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n/an/a 194n/an/an/an/an/an/a



Wyeth-Ayerst Research



Assay Description
The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...


J Med Chem 44: 2719-34 (2001)


Article DOI: 10.1021/jm0005555
BindingDB Entry DOI: 10.7270/Q2PN93TS
More data for this
Ligand-Target Pair
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