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Ephrin type-A receptor 2 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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Lithocholic acidIC5050000.0 [1], 57543.99 [2]
Glycolithocholic acidIC5048977.88 [1], 138000.0 [2]
CID 71718651IC502041.74 [1], 2200.0 [2]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1H-indol-3-yl)propanoic acidIC503548.13 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1H-indol-3-yl)propanoic acidKi1400.0 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(5-hydroxy-1H-indol-3-yl)propanoic acidIC506025.6 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(5-hydroxy-1H-indol-3-yl)propanoic acidKi2400.0 [1]
(2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]propanoic acidIC5019952.62 [1], 79000.0 [2]
(2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-methylbutanoic acidIC5023988.33 [1], 71000.0 [2]
(2S)-3-Hydroxy-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]propanoic acidIC5033113.11 [1], 101000.0 [2]
(2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-4-methylsulfanylbutanoic acidIC5026000.0 [1], 27542.29 [2]
(2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-phenylpropanoic acidIC506606.93 [1], 19000.0 [2]
(2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(4-hydroxyphenyl)propanoic acidIC5050118.72 [1], 98000.0 [2]
StaurosporineIC50262.6 [1]
DasatinibIC50137.0 [1]
CrizotinibIC501000.0 [1]
IbrutinibIC501000.0 [1]
DorsomorphinIC5011.0 [1]
DoramapimodIC50160.0 [1]
3b-Hydroxy-5-cholenoic acidIC5039810.72 [1]
LY-3009120IC5020.0 [1]
TesevatinibIC5050.0 [1]
1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanoneIC50760.0 [1]
Nms-P937 (nms1286937)IC5010000.0 [1]
CID 59604787IC5010000.0 [1]
CID 44478401IC502.3 [1]
2-[1-(4,4-Difluorocyclohexyl)-piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamideIC5010000.0 [1]
4-Amino-5-chloro-6-ethoxy-pyridine-2-carboxylic acid 4-methanesulfonyl-benzylamideKi8000.0 [1]
7-Chloro-3-oxo-8-(1,3-thiazol-5-ylmethylamino)-11,16-dioxa-2,4,19,21-tetrazatricyclo[15.3.1.05,10]henicosa-1(20),5,7,9,17(21),18-hexaene-18-carbonitrileKi8000.0 [1]
1-({4-[(3,4-Dichlorophenyl)methoxy]phenyl}methyl)azetidine-3-carboxylic acidIC5010000.0 [1]
4-[(2-Morpholin-4-yl-7H-purin-6-yl)amino]benzenesulfonamideIC5010000.0 [1]
4-[2-[4-(3-Pyridin-4-ylpyrazolo[1,5-a]pyrimidin-6-yl)phenoxy]ethyl]morpholineIC50250.0 [1]
7-Chloro-8-(3-hydroxypropoxy)-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5,7,9,18(22),19-hexaene-19-carbonitrileKi10000.0 [1]
7-Chloro-8-(3-hydroxypropyl)-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5(10),6,8,18(22),19-hexaene-19-carbonitrileKi10000.0 [1]
N-(7-Chloro-19-cyano-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5,7,9,18(22),19-hexaen-8-yl)methanesulfonamideKi10000.0 [1]
Ripk1-IN-7IC50341.0 [1]
(3S)-3-[[(4R)-4-[(5S,8R,9S,10S,13R,14S,17R)-10,13-Dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-4-(1H-indol-3-yl)butanoic acidKi15000.0 [1]
[6-Chloro-4-methyl-3-[[3-(methylsulfamoylamino)phenyl]methyl]-2-oxochromen-7-yl] N,N-dimethylcarbamateIC5050000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acidIC504100.0 [1]
5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamideIC5010000.0 [1]
5-(2-Aminoethyl)-7-(7-(benzo[b]thiophen-2-yl)-1H-indazol-5-yl)-5H-pyrrolo[3,2-d]pyrimidin-2-amineIC5010000.0 [1]
CID 46864270IC500.6 [1]
N-[3-[5-[2-(3-Morpholin-4-ylanilino)pyrimidin-4-yl]imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-phenylacetamideIC50370.0 [1]
3-(2-Aminopropan-2-yl)-N-[(2R)-7-[(7-oxo-6,8-dihydro-5H-1,8-naphthyridin-4-yl)oxy]-1,2,3,4-tetrahydronaphthalen-2-yl]-5-(trifluoromethyl)benzamideIC5011.0 [1]
3-(4-Acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-(trifluoromethyl)quinolineIC5010000.0 [1]
Ethyl 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carboxylateIC5010000.0 [1]
1-(4-Fluorophenyl)-N-[3-fluoro-4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)oxyphenyl]-2-oxopyridine-3-carboxamideIC5010000.0 [1]
1-[5-Tert-butyl-3-[4-[2-(dimethylamino)ethyl]-5-oxo-1,4-diazepane-1-carbonyl]thiophen-2-yl]-3-(2,3-dichlorophenyl)ureaIC5016000.0 [1]
N-(7-Methoxyquinolin-6-yl)thieno[3,2-d]pyrimidine-7-carboxamideIC5050000.0 [1]
CID 67161540IC501700.0 [1]
6-(2,4-Difluorophenyl)sulfonyl-2-(1H-indol-5-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-oneIC5010000.0 [1]
CID 71553154IC502430.0 [1]
6-(6-Fluoroindol-1-yl)-2-[2-[7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyethyl]pyridazin-3-oneIC501000.0 [1]
3-Amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamideIC507000.0 [1]
(2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]butanedioic acidIC50316227.77 [1]
3-Amino-6-(piperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamideIC507000.0 [1]
1-[3-[8-(Pyridin-4-ylmethylamino)imidazo[1,2-a]pyrazin-6-yl]phenyl]-3-[3-(trifluoromethyl)phenyl]ureaIC5035.0 [1]
3-[[5-(1,3-Benzodioxol-5-yl)-[1,2,4]triazolo[1,5-c]quinazolin-8-yl]amino]propan-1-olIC5010000.0 [1]
Tert-butyl 2-[[4-(3-chloroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]morpholine-4-carboxylateIC501190.0 [1]
N-(3-Chlorophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amineIC501470.0 [1]
Tert-butyl 2-[[4-(3-bromoanilino)-6-methoxyquinazolin-7-yl]oxymethyl]morpholine-4-carboxylateIC502500.0 [1]
N-(3-Bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amineIC50750.0 [1]
Tert-butyl 2-[[4-(4-bromoanilino)-6-methoxyquinazolin-7-yl]oxymethyl]morpholine-4-carboxylateIC502310.0 [1]
N-(4-Bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amineIC50680.0 [1]
N-(3-Chlorophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50580.0 [1]
N-(3-Bromophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50730.0 [1]
N-(4-Bromophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50720.0 [1]
N-(4-Fluorophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50620.0 [1]
N-(3,5-Dichlorophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50960.0 [1]
N-[4-Fluoro-3-(trifluoromethyl)phenyl]-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC503210.0 [1]
N-(4-Fluoro-2-methylphenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50200.0 [1]
N-[4-Chloro-3-(trifluoromethyl)phenyl]-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50170.0 [1]
N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50450.0 [1]
N-(4-Bromo-2-chlorophenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50230.0 [1]
N-(4-Bromo-3-methylphenyl)-6-methoxy-7-(morpholin-2-ylmethoxy)quinazolin-4-amineIC50320.0 [1]
3-[2-(4-Amino-1-ethylpyrazolo[3,4-d]pyrimidin-3-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamideIC5016.0 [1]
6-(1-Methylpyrazol-4-yl)-2-[[3-[[5-(1-methylpyrazol-4-yl)pyrimidin-2-yl]amino]phenyl]methyl]pyridazin-3-oneIC501000.0 [1]
(3S)-3-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-4-(1H-indol-3-yl)butanoic acidIC504265.8 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Acetyloxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1H-indol-3-yl)propanoic acidIC5089125.09 [1]
(3S)-2-[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Acetyloxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]-1,3,4,9-tetrahydropyrido[3,4-b]indole-3-carboxylic acidIC506309.57 [1]
(2S)-3-(5-Fluoro-1H-indol-3-yl)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]propanoic acidIC508912.51 [1]
(2S)-3-Hydroxy-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]propanoic acidIC50100000.0 [1]
(2R)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1H-indol-3-yl)propanoic acidIC50100000.0 [1]
(2S)-3-(5-Bromo-1H-indol-3-yl)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]propanoic acidIC5022387.21 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(5-methoxy-1H-indol-3-yl)propanoic acidIC5047863.01 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-phenylpropanoic acidIC50100000.0 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-phenoxypropanoic acidIC5050118.72 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1-methylindol-3-yl)propanoic acidIC505011.87 [1]
(2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-naphthalen-1-ylpropanoic acidIC504073.8 [1]
N-[1-(3-Chlorophenyl)ethyl]-3-pyridin-4-yl-1H-indazole-5-carboxamideIC501000.0 [1]
N-[1-(3,5-Dichloropyridin-4-yl)ethyl]-3-(2-methylpyridin-4-yl)-1H-indazole-5-carboxamideIC501000.0 [1]
9-Ethyl-8-[4-[(4-hydroxyoxan-4-yl)methyl]piperazin-1-yl]-6,6-dimethyl-11-oxo-5H-benzo[b]carbazole-3-carbonitrileIC501000.0 [1]
c-Met-IN-2IC5030000.0 [1]
2-[5-[(1R)-1-(3,5-Dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]-6-(4-methylpiperazin-1-yl)-1H-benzimidazoleIC50100.0 [1]
4-Chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-isoquinolin-6-ylpyridin-2-yl]phenolIC50100.0 [1]
4-Fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenolIC5010.0 [1]
5-Fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenolIC50100.0 [1]
4-Chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenolIC5010.0 [1]
N-Methyl-6-[2-[[4-(4-methylpiperazin-1-yl)benzoyl]amino]pyridin-4-yl]oxynaphthalene-1-carboxamideIC501000.0 [1]
N-[(7S)-4-Amino-6-methylidene-5-(4-phenoxyphenyl)-7,8-dihydropyrimido[5,4-b]pyrrolizin-7-yl]prop-2-enamideIC501000.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Ephrin type-A receptor 2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/ephrin-type-a-receptor-2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ Ephrin type-A receptor 2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/ephrin-type-a-receptor-2-inhibitors-ic50-ki.
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