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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