Target Validation Information
Target ID T80975
Target Name Vascular endothelial growth factor receptor 2
Target Type
Successful
Drug Potency against Target (3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 1410 nM [527458]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info IC50 = 14400 nM [527458]
4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 6300 nM [527245]
4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Drug Info IC50 = 15000 nM [527245]
AZD-1152-HQPA Drug Info Ki = 1800 nM [528741]
CEP-11981 Drug Info Ki = 18 nM [552381]
3-((3-bromothiophen-2-yl)methylene)indolin-2-one Drug Info IC50 = 15400 nM [528681]
HKI-272 Drug Info IC50 = 858.2 nM [528774]
Brivanib Drug Info Ki = 28 nM [528103]
VATALANIB Drug Info IC50 = 30 nM [552881]
3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info IC50 = 7600 nM [527458]
(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 3260 nM [527458]
SU-11652 Drug Info IC50 = 50 nM [526575]
Phenyl-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 3000 nM [527458]
[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Drug Info IC50 = 1650 nM [527458]
TG-100435 Drug Info Ki = 784 nM [528527]
Axitinib Drug Info IC50 = 0.2 nM [552885]
XL880 Drug Info Ki = 0.86 nM [552987]
SU-14813 Drug Info IC50 = 50 nM [552773]
4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Drug Info IC50 = 11000 nM [527245]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info IC50 = 3300 nM [528122]
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Drug Info IC50 = 224 nM [526462]
L000021649 Drug Info IC50 = 3 nM [526462]
Ro-4396686 Drug Info IC50 = 50 nM [528018]
2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile Drug Info IC50 = 1000 nM [528821]
Vandetanib Drug Info IC50 = 40 nM [552828]
Sunitinib Drug Info Ki = 80 nM [552892]
4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile Drug Info IC50 = 1000 nM [528821]
AG1295 Drug Info IC50 = 6200 nM [530377]
WHI-P180 Drug Info IC50 = 50 nM [528681]
CP-547632 Drug Info IC50 = 11 nM [552306]
8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one Drug Info IC50 = 1000 nM [528681]
OSI-930 Drug Info Ki = 9 nM [552540]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine Drug Info IC50 = 2720 nM [525876]
CB-676475 Drug Info IC50 = 1000 nM [527794]
Motesanib Drug Info Ki = 3 nM [552634]
3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine Drug Info IC50 = 4900 nM [528593]
IM-023911 Drug Info IC50 = 190 nM [527725]
4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide Drug Info IC50 = 1600 nM [527725]
3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole Drug Info IC50 = 126 nM [526703]
SU-6668 Drug Info Ki = 2100 nM [552226]
3-(1H-Indol-2-yl)-1H-quinolin-2-one Drug Info IC50 = 8 nM [526914]
6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one Drug Info IC50 = 355 nM [526914]
4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide Drug Info IC50 = 1800 nM [527725]
4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info IC50 = 4790 nM [528716]
PD-153035 Drug Info IC50 = 1489 nM [528774]
3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole Drug Info IC50 = 1200 nM [528227]
VATALANIB Drug Info IC50 = 6754 nM [528774]
BMS-536924 Drug Info IC50 = 1400 nM [527711]
CEP-5104 Drug Info IC50 = 4175 nM [529647]
BAY-57-9352 Drug Info Ki = 6 nM [552978]
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info IC50 = 1700 nM [529891]
4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Drug Info IC50 = 4660 nM [527458]
N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Drug Info IC50 = 15000 nM [527245]
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine Drug Info IC50 = 1700 nM [527458]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 14000 nM [527245]
N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 530 nM [527245]
4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 14000 nM [527245]
Isoindolinone Urea derivative Drug Info IC50 = 18 nM [527209]
BMS-645737 Drug Info IC50 = 53 nM [529409]
Cediranib Drug Info IC50 < 1 nM [552727]
6-o-tolylquinazolin-2-amine Drug Info IC50 = 4966 nM [528429]
3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide Drug Info IC50 = 17000 nM [527793]
5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole Drug Info IC50 = 113 nM [526669]
2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile Drug Info IC50 = 990 nM [527935]
KRN633 Drug Info IC50 = 1.16 nM [527373]
Action against Disease Model Sunitinib In nine h uMan AML cell lines, sunitinib were potent inhibitor of cellular proliferation (IC50: 7~13,000 nM/L) [552819] Drug Info
References
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Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
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