Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T59328 | ||||
Target Name | Epidermal growth factor receptor | ||||
Target Type | Successful |
||||
Drug Potency against Target | Tyverb/Tykerb | Drug Info | Ki = 10.8 nM | [553160] | |
Gefitinib | Drug Info | IC50 = 2.1 nM | [552495] | ||
TAK165 | Drug Info | IC50 = 25000 nM | [552607] | ||
4-(2-nitrovinyl)benzene-1,2-diol | Drug Info | IC50 = 9000 nM | |||
AEE-788 | Drug Info | IC50 = 6 nM | [552727] | ||
RG-50810 | Drug Info | IC50 = 10000 nM | |||
AG-538 | Drug Info | IC50 = 400 nM | |||
Erlotinib | Drug Info | IC50 = 2.7 nM | [552495] | ||
N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine | Drug Info | IC50 = 0.12 nM | [534127] | ||
(3-Bromo-phenyl)-quinazolin-4-yl-amine | Drug Info | IC50 = 27 nM | [534127] | ||
PD-153035 | Drug Info | IC50 = 200 nM | [530858] | ||
6,7-dimethoxy-N-m-tolylquinazolin-4-amine | Drug Info | IC50 = 4.6 nM | [529935] | ||
PD-158780 | Drug Info | IC50 = 15 nM | [534120] | ||
PD-0180970 | Drug Info | IC50 = 390 nM | [525862] | ||
(E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin | Drug Info | IC50 = 19000 nM | [530002] | ||
CGP-53353 | Drug Info | IC50 = 2200 nM | [533915] | ||
5,6-Bis-p-tolylamino-isoindole-1,3-dione | Drug Info | IC50 = 4500 nM | [533915] | ||
BMS-599626 | Drug Info | Ki = 22 nM | [552652] | ||
N4-(3-chlorophenyl)quinazoline-4,6-diamine | Drug Info | IC50 = 200 nM | [528809] | ||
N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine | Drug Info | IC50 = 2085 nM | [534120] | ||
BIBW 2992 | Drug Info | Ki = 0.5 nM | [552665] | ||
PD-0173956 | Drug Info | IC50 = 380 nM | [525862] | ||
PD-168393 | Drug Info | IC50 < 1 nM | [528707] | ||
N-(4-(phenylamino)quinazolin-6-yl)acrylamide | Drug Info | IC50 < 1 nM | [528707] | ||
CI-1033 | Drug Info | IC50 = 0.8 nM | [552773] | ||
AG-213 | Drug Info | IC50 = 1310 nM | [529134] | ||
4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline | Drug Info | IC50 = 131 nM | [529134] | ||
N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide | Drug Info | IC50 = 90 nM | [525502] | ||
4-(3-Bromo-phenylamino)-quinazoline-6,7-diol | Drug Info | IC50 = 0.17 nM | [534127] | ||
N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine | Drug Info | IC50 = 40 nM | [526895] | ||
2-methoxy-4-(2-nitrovinyl)phenol | Drug Info | IC50 = 8000 nM | |||
Lapatinib | Drug Info | Ki = 10.8 nM | [552318] | ||
HKI-272 | Drug Info | IC50 = 0.18 nM | [528774] | ||
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline | Drug Info | IC50 = 70 nM | |||
N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide | Drug Info | IC50 = 4.7 nM | [525502] | ||
6,7-dimethoxy-4-(2-phenylethynyl)quinazoline | Drug Info | IC50 = 5600 nM | [529046] | ||
6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline | Drug Info | IC50 = 14 nM | [529046] | ||
6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline | Drug Info | IC50 = 15 nM | [529046] | ||
6,7-diethoxy-4-styrylquinazoline | Drug Info | IC50 = 15 nM | [529046] | ||
4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline | Drug Info | IC50 = 26 nM | [529046] | ||
(3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine | Drug Info | IC50 = 355 nM | [533683] | ||
VATALANIB | Drug Info | IC50 = 457.7 nM | [528774] | ||
PD-0166326 | Drug Info | IC50 = 82 nM | [525862] | ||
Cetuximab | Drug Info | IC50 = 150 nM | [552482] | ||
HTS-00213 | Drug Info | IC50 = 6300 nM | [529935] | ||
6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline | Drug Info | IC50 = 140 nM | [529046] | ||
CL-387785 | Drug Info | IC50 = 8 nM | [529935] | ||
N4-(3-methylphenyl)-4,6-quinazolinediamine | Drug Info | IC50 = 1000 nM | [528236] | ||
Vandetanib | Drug Info | IC50 = 500 nM | [552773] | ||
2-cyano-3-(3,4-dihydroxyphenyl)acrylamide | Drug Info | IC50 = 10000 nM | |||
N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine | Drug Info | IC50 = 0.1 nM | [533683] | ||
3-Pyridin-4-yl-quinoline-6,7-diol | Drug Info | IC50 = 5000 nM | [533872] | ||
Lapatinib | Drug Info | IC50 = 3 nM | [552773] | ||
4-(2-nitroprop-1-enyl)benzene-1,2-diol | Drug Info | IC50 = 9000 nM | |||
Benzyl-quinazolin-4-yl-amine | Drug Info | IC50 = 320 nM | [533683] | ||
Ro-4396686 | Drug Info | IC50 = 545 nM | [528018] | ||
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | IC50 = 2500 nM | |||
6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline | Drug Info | IC50 = 5 nM | [529046] | ||
4-(2-nitrovinyl)phenol | Drug Info | IC50 = 10000 nM | |||
3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one | Drug Info | IC50 = 16000 nM | [525445] | ||
TYRPHOSTIN AG-1478 | Drug Info | IC50 < 100 nM | [525445] | ||
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine | Drug Info | IC50 = 2700 nM | [530473] | ||
10-hydroxy-18-methoxybetaenone | Drug Info | IC50 = 10500 nM | [525806] | ||
2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile | Drug Info | IC50 = 500 nM | [528244] | ||
2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile | Drug Info | IC50 = 7000 nM | [528244] | ||
4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid | Drug Info | IC50 = 1000 nM | |||
LAVENDUSTIN A | Drug Info | IC50 = 4100 nM | [533837] | ||
2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile | Drug Info | IC50 = 1000 nM | |||
Cochliobolic acid | Drug Info | IC50 = 1600 nM | [534313] | ||
HKI-272 | Drug Info | IC50 = 59 nM | [552828] | ||
SKI-758 | Drug Info | IC50 = 230 nM | [528584] | ||
References | |||||
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Ref 525862 | Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. | ||||
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Ref 552665 | Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). Eur J Cancer. 2007 Feb;43(3):481-9. Epub 2007 Jan 8. | ||||
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Ref 525445 | J Med Chem. 1999 Mar 25;42(6):1018-26.Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. | ||||
Ref 525445 | J Med Chem. 1999 Mar 25;42(6):1018-26.Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. | ||||
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Ref 528244 | J Med Chem. 1991 Jun;34(6):1896-907.Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. | ||||
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Ref 528584 | J Med Chem. 2006 Dec 28;49(26):7868-76.Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. |
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