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Vascular endothelial growth factor receptor 1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
VatalanibIC50140.0 [1]
2-(Pyridin-4-Ylmethylamino)-~{n}-[3-(Trifluoromethyl)phenyl]benzamideIC50170.0 [1]
N-(4-Chloro-2-fluorophenyl)-6,7-dimethoxyquinazolin-4-amineIC5014100.0 [1]
VandetanibIC50100.0 [1]
StaurosporineIC505.4 [1], 8.19 [2], 15.97 [3], 19.0 [4], 35.0 [5]
2-{[(Pyridin-4-yl)methyl]amino}-N-(quinolin-3-yl)benzamideIC5015.0 [1], 160.0 [2]
SemaxanibIC508.0 [1], 43.0 [2], 3000.0 [3]
LinifanibIC503.0 [1], 37.0 [2], 70.0 [3]
(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]pentanediamideIC50102700.0 [1], 160000.0 [2]
SorafenibIC5018.0 [1], 31.0 [2], 165.0 [3]
NintedanibIC5023.4 [1], 34.0 [2], 104.0 [3]
ForetinibIC500.8 [1], 6.8 [2]
N4-(3-Bromophenyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC5016000.0 [1], 19200.0 [2]
4-N-(3-Bromophenyl)-6-[(2-methylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC5050000.0 [1]
4-N-(3-Bromophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC5031100.0 [1], 45900.0 [2]
c[YYDEGLEE]-NH2IC5023000.0 [1], 32000.0 [2], 39900.0 [3]
SunitinibIC501.0 [1]
SunitinibKi2.0 [1]
PazopanibIC5010.0 [1], 98.0 [2]
DovitinibIC503.0 [1], 10.0 [2]
MotesanibIC502.0 [1]
TivozanibIC500.21 [1], 6.26 [2]
VEGF receptor tyrosine kinase inhibitor IIIIC501.0 [1], 170.0 [2]
LucitanibIC507.0 [1]
N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[2-(triazol-1-yl)ethoxy]quinazolin-4-amineIC50700.0 [1]
IlorasertibIC501.25 [1], 32.0 [2]
Tak-593IC503.2 [1]
3-(4-{4-Aminofuro[2,3-d]pyrimidin-5-yl}phenyl)-1-[2-fluoro-5-(trifluoromethyl)phenyl]ureaIC507.76 [1], 8.51 [2]
1-[4-(4-Aminothieno[2,3-d]pyrimidin-5-yl)phenyl]-3-(3-methylphenyl)ureaIC502.0 [1]
2-Benzyl-N4-(3-bromophenyl)-1H-indole-4,6-diamineIC5050000.0 [1]
6-(2-Phenylethyl)-4-N-[3-(trifluoromethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC50200000.0 [1]
2-(2-Chlorobenzyl)-N4-(3-bromophenyl)-1H-indole-4,6-diamineIC5026800.0 [1]
N-(4-Chloro-2-fluorophenyl)-6-methoxy-7-(2-methoxyethoxy)quinazolin-4-amineIC50400.0 [1]
4-N-(3-Bromo-4-fluorophenyl)-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC50200000.0 [1]
1-Methyl-1-[[5-[7-[(4-methylpiperazin-1-yl)methyl]-2,4-dihydroindeno[1,2-c]pyrazol-3-yl]thiophen-2-yl]methyl]-3-[3-(trifluoromethyl)phenyl]ureaIC5014.0 [1]
(4S)-5-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-Amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-oxopentanoic acidIC5028000.0 [1]
4-N-[4-Fluoro-3-(trifluoromethyl)phenyl]-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC50200000.0 [1]
4-N-(3-Bromophenyl)-6-[(2,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC5050000.0 [1]
N4-(3-Bromophenyl)-2-(naphthalen-2-ylmethyl)-1H-indole-4,6-diamineIC5015200.0 [1]
N4-(3-Bromophenyl)-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC5045100.0 [1]
4-N-(3-Ethynylphenyl)-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC50200000.0 [1]
4-N-(4-Chloro-2-fluorophenyl)-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC50200000.0 [1]
N4-1H-Indol-5-yl-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamineIC50200000.0 [1]
Anilinoquinazoline deriv. 21IC501100.0 [1]
Anilinoquinazoline deriv. 22IC50200.0 [1]
Anilinoquinazoline deriv. 28IC50100.0 [1]
Anilinoquinazoline deriv. 32IC501500.0 [1], 15000.0 [2]
N-[4-[(4-Methylpiperazin-1-yl)methyl]phenyl]-4-(thieno[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamideIC5019.8 [1]
c[YYAEGLEE]-NH2IC5025000.0 [1], 35000.0 [2]
3-[(3S,6S,9S,12S,15S,18S,21S,26S)-26-Carbamoyl-12-(2-carboxyethyl)-15-(carboxymethyl)-18,21-bis[(4-hydroxyphenyl)methyl]-9-methyl-6-(2-methylpropyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclohexacos-3-yl]propanoic acidIC50101000.0 [1], 105000.0 [2]
(3R,6S,9S,14S,17S,23S,26S)-9-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]-3-(4-aminobutyl)-N-[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]-17-(3-amino-3-oxopropyl)-6-[(2S)-butan-2-yl]-23-(1H-imidazol-5-ylmethyl)-2,5,8,16,19,22,25-heptaoxo-1,4,7,15,18,21,24-heptazabicyclo[24.3.0]nonacosane-14-carboxamideIC5091600.0 [1], 105500.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]pent-4-enoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1-oxopent-4-en-2-yl]pentanediamideIC5036500.0 [1], 42300.0 [2]
(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]pent-4-enoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1-oxopent-4-en-2-yl]pentanediamideIC5061200.0 [1], 61800.0 [2]
(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamidopent-4-enoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S)-1-amino-1-oxopent-4-en-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]pentanediamideIC5076800.0 [1], 98800.0 [2]
(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]pent-4-enoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1-oxopent-4-en-2-yl]pentanediamideIC5090300.0 [1], 109500.0 [2]
(3S,6S,9S,14S,17S,23S,26S,29S)-9-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]-3-(4-aminobutyl)-N-[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]-17,23-bis(3-amino-3-oxopropyl)-6-[(2S)-butan-2-yl]-26-(1H-imidazol-5-ylmethyl)-2,5,8,12,16,19,22,25,28-nonaoxo-1,4,7,11,15,18,21,24,27-nonazabicyclo[27.3.0]dotriacontane-14-carboxamideIC5087600.0 [1], 93200.0 [2]
Methyl (2S,4R)-1-[3-[[7-[4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propyl]-4-hydroxypyrrolidine-2-carboxylateIC5010.0 [1], 15.0 [2]
N-[2-(Diethylamino)ethyl]-7-[4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carboxamideIC505.0 [1], 13.0 [2]
N-[3-(Diethylamino)propyl]-7-[4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carboxamideIC503.0 [1], 12.0 [2]
7-[4-[(2-Fluoro-5-methylphenyl)carbamoylamino]phenoxy]-N-[3-(2H-tetrazol-5-yl)propyl]thieno[3,2-b]pyridine-2-carboxamideIC504.0 [1], 20.0 [2]
7-[4-[(2-Fluoro-5-methylphenyl)carbamoylamino]phenoxy]-N-[2-(2H-tetrazol-5-yl)ethyl]thieno[3,2-b]pyridine-2-carboxamideIC5010.0 [1], 19.0 [2]
Ethyl 2-[4-[3-[[7-[4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propyl]piperazin-1-yl]acetateIC505.0 [1], 13.0 [2]
7-[4-[(2-Fluoro-5-methylphenyl)carbamoylamino]phenoxy]-N-[3-[3-(hydroxymethyl)piperidin-1-yl]propyl]thieno[3,2-b]pyridine-2-carboxamideIC503.0 [1], 10.0 [2]
7-[4-[(2-Fluoro-5-methylphenyl)carbamoylamino]phenoxy]-N-[3-[2-(hydroxymethyl)morpholin-4-yl]propyl]thieno[3,2-b]pyridine-2-carboxamideIC5010.0 [1], 15.0 [2]
Methyl 2-[3-[[7-[4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propylamino]acetateIC506.0 [1], 11.0 [2]
Methyl 2-[3-[[7-[4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propyl-(2-methoxy-2-oxoethyl)amino]acetateIC509.0 [1], 14.0 [2]
Ethyl 4-[2-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]ethyl]piperazine-1-carboxylateIC5013.0 [1], 14.0 [2]
Ethyl 4-[3-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propyl]piperazine-1-carboxylateIC509.0 [1], 14.0 [2]
Methyl 2-[3-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propylamino]acetateIC508.0 [1], 11.0 [2]
Methyl 2-[3-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]propyl-(2-methoxy-2-oxoethyl)amino]acetateIC5010.0 [1], 12.0 [2]
Methyl 2-[2-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]ethyl-(2-methoxy-2-oxoethyl)amino]acetateIC5011.0 [1], 17.0 [2]
Methyl 1-[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]pyrrolidine-3-carboxylateIC508.0 [1], 17.0 [2]
Ethyl 2-[4-[2-[4-[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]piperazin-1-yl]acetyl]piperazin-1-yl]acetateIC5010.0 [1], 13.0 [2]
Ethyl 2-[4-[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]piperazin-1-yl]acetateIC5017.0 [1], 112.0 [2]
Methyl 2-[2-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]ethylamino]acetateIC509.0 [1], 13.0 [2]
N-(2-Aminoethyl)-7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carboxamideIC5011.0 [1], 15.0 [2]
Tert-butyl N-[2-[[7-[3-fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]thieno[3,2-b]pyridine-2-carbonyl]amino]ethyl]carbamateIC5060.0 [1], 69.0 [2]
7-[3-Fluoro-4-[(2-fluoro-5-methylphenyl)carbamoylamino]phenoxy]-N-[3-(4-methylpiperazin-1-yl)propyl]thieno[3,2-b]pyridine-2-carboxamideIC506.0 [1], 11.0 [2]
2,3,7,8-Tetrachlorodibenzo-P-dioxinKi0.7 [1]
ErlotinibIC501000.0 [1]
HematoxylineIC502900.0 [1]
DigitinKi1001.0 [1]
CrizotinibIC501000.0 [1]
DorsomorphinIC5011.0 [1]
AxitinibIC500.1 [1]
Nintedanib esylateIC5034.0 [1]
CediranibIC505.0 [1]
CabozantinibIC5012.0 [1]
PonatinibIC5020.9 [1]
Chir-99021IC505000.0 [1]
SaracatinibIC50100000.0 [1]
DoramapimodIC50250.0 [1]
QuizartinibIC5010000.0 [1]
OrantinibIC5028.0 [1]
BrivanibKi60.0 [1]
3,9-Bis((ethylthio)methyl)-K-252aIC50209.0 [1]
Nvp-tae 684IC50872.0 [1]
(R)-6-(4-((4-Ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineIC5059.0 [1]
Pyridone 6IC501520.0 [1]
1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)ureaIC5010.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Vascular endothelial growth factor receptor 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/vascular-endothelial-growth-factor-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Vascular endothelial growth factor receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/vascular-endothelial-growth-factor-receptor-1-inhibitors-ic50-ki.
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