Target Validation Information
TTD ID T80975
Target Name Vascular endothelial growth factor receptor 2 (KDR)
Type of Target
Successful
Drug Potency against Target Sunitinib Drug Info Ki = 80 nM [43]
Axitinib Drug Info IC50 = 0.2 nM [42]
BAY-57-9352 Drug Info Ki = 6 nM [44]
Cediranib Drug Info IC50 < 1 nM [37]
CEP-11981 Drug Info Ki = 18 nM [34]
CP-547632 Drug Info IC50 = 11 nM [33]
KRN633 Drug Info IC50 = 1.16 nM [9]
Motesanib Drug Info Ki = 3 nM [36]
OSI-930 Drug Info Ki = 9 nM [35]
Rosiglitazone + metformin Drug Info Ki = 2100 nM [32]
SU-14813 Drug Info IC50 = 50 nM [38]
Vandetanib Drug Info IC50 = 40 nM [40]
VATALANIB Drug Info IC50 = 30 nM [41]
XL880 Drug Info Ki = 0.86 nM [45]
(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 3260 nM [10]
(3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 1410 nM [10]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine Drug Info IC50 = 2720 nM [1]
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine Drug Info IC50 = 1700 nM [10]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info IC50 = 3300 nM [18]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info IC50 = 14400 nM [10]
2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile Drug Info IC50 = 1000 nM [27]
2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile Drug Info IC50 = 990 nM [15]
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Drug Info IC50 = 224 nM [2]
3-((3-bromothiophen-2-yl)methylene)indolin-2-one Drug Info IC50 = 15400 nM [23]
3-(1H-Indol-2-yl)-1H-quinolin-2-one Drug Info IC50 = 8 nM [6]
3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine Drug Info IC50 = 4900 nM [22]
3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info IC50 = 7600 nM [10]
3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole Drug Info IC50 = 126 nM [5]
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info IC50 = 1700 nM [30]
3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide Drug Info IC50 = 17000 nM [13]
3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole Drug Info IC50 = 1200 nM [19]
4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info IC50 = 4790 nM [24]
4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide Drug Info IC50 = 1600 nM [12]
4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide Drug Info IC50 = 1800 nM [12]
4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Drug Info IC50 = 4660 nM [10]
4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 14000 nM [8]
4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Drug Info IC50 = 15000 nM [8]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 14000 nM [8]
4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 6300 nM [8]
4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Drug Info IC50 = 11000 nM [8]
4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile Drug Info IC50 = 1000 nM [27]
4-[3-Hydroxyanilino]-6,7-Dimethoxyquinazoline Drug Info IC50 = 50 nM [23]
5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole Drug Info IC50 = 113 nM [4]
6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one Drug Info IC50 = 355 nM [6]
6-o-tolylquinazolin-2-amine Drug Info IC50 = 4966 nM [20]
8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one Drug Info IC50 = 1000 nM [23]
AG1295 Drug Info IC50 = 6200 nM [31]
AZD-1152-HQPA Drug Info Ki = 1800 nM [25]
BMS-536924 Drug Info IC50 = 1400 nM [11]
BMS-645737 Drug Info IC50 = 53 nM [28]
Brivanib Drug Info Ki = 28 nM [17]
CB-676475 Drug Info IC50 = 1000 nM [14]
CEP-5104 Drug Info IC50 = 4175 nM [29]
HKI-272 Drug Info IC50 = 858.2 nM [26]
IM-023911 Drug Info IC50 = 190 nM [12]
Isoindolinone Urea derivative Drug Info IC50 = 18 nM [7]
L000021649 Drug Info IC50 = 3 nM [2]
N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 530 nM [8]
N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Drug Info IC50 = 15000 nM [8]
PD-153035 Drug Info IC50 = 1489 nM [26]
Phenyl-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 3000 nM [10]
Ro-4396686 Drug Info IC50 = 50 nM [16]
SU-11652 Drug Info IC50 = 50 nM [3]
TG-100435 Drug Info Ki = 784 nM [21]
VATALANIB Drug Info IC50 = 6754 nM [26]
[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Drug Info IC50 = 1650 nM [10]
Action against Disease Model Sunitinib Drug Info In nine h uMan AML cell lines, sunitinib were potent inhibitor of cellular proliferation (IC50: 7~13,000 nM/L) [39]
References
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