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Nerve growth factor receptor Trk-A 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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StaurosporineIC500.5 [1], 1.29 [2], 1.7 [3], 3.1 [4], 8.3 [5]
N-(5-Cyclopropyl-2-phenylpyrazol-3-yl)-2-[4-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamideIC5047.0 [1], 85.4 [2], 119.3 [3], 287.2 [4], 662.0 [5]
Antibiotic K 252aIC502.4 [1], 13.0 [2]
Methyl (15S,16S,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylateIC501.2 [1], 5.0 [2]
AZ-23IC503.2 [1], 8.9 [2], 9.9 [3]
1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-oneIC502.0 [1], 3.0 [2]
1H-Benz(de)isoquinoline-1,3(2H)-dione, 2-((2-hydroxyethyl)amino)-5-nitro-IC503720.0 [1], 5880.0 [2], 149000.0 [3]
(R)-3-((6,7,8,9-Tetrahydro-5H-benzo[7]annulen-5-yl)thio)-5-ureidoisothiazole-4-carboxamideIC501.0 [1], 7.0 [2]
1-[(3S,4R)-4-(3,4-Difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl]-3-(5-ethoxy-4-methyl-2-phenylpyrazol-3-yl)ureaIC502.7 [1], 6.0 [2], 37163.3 [3]
2-[4-[4-[6-[(2R)-2-(3-Fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acidIC501.0 [1]
1-[4-[6-[(2R)-2-(3-Fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-olIC503.0 [1], 4.0 [2], 10.0 [3]
5-[[2-Chloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-(3-hydroxycyclobutyl)-1-phenylpyrazole-3-carboxamideIC5061.8 [1], 75.8 [2], 82.2 [3]
CrizotinibIC501.0 [1], 580.0 [2]
Purvalanol BIC5051.0 [1], 1710.0 [2]
LarotrectinibIC509.7 [1]
EntrectinibIC501.0 [1], 3.0 [2]
JNJ-28312141 free baseIC5015.0 [1], 150.0 [2]
4-[2-(Butylamino)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexan-1-olIC501.67 [1]
2-Amino-1-[4-[5-[[2-[(6-bromopyridin-2-yl)amino]-1,3-thiazol-5-yl]sulfanyl]-2-methylbenzoyl]piperazin-1-yl]ethanoneIC500.6 [1]
CID 59627005IC501.4 [1], 3.0 [2]
1-Propan-2-yl-1-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-3-[4-(trifluoromethoxy)phenyl]ureaIC503.0 [1], 11.0 [2]
3-{[(4-Chlorophenyl)methyl]sulfanyl}-5-(pyridin-3-ylamino)-1,2-thiazole-4-carboxamideIC5019.0 [1], 581.0 [2]
3-{[(4-Chlorophenyl)methyl]sulfanyl}-5-[(6-methoxypyridin-3-yl)amino]-1,2-thiazole-4-carboxamideIC50179.0 [1], 1000.0 [2]
(15S,16S,18R)-16-Hydroxy-15,16-dimethyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-oneIC503.0 [1], 10.0 [2]
5-Cyano-N-[2-(cyclohexen-1-yl)-4-[1-(2-methylsulfonylethyl)piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamideIC5030.0 [1], 500.0 [2]
3-{[(4-Chlorophenyl)methyl]sulfanyl}-5-(pyridin-2-ylamino)-1,2-thiazole-4-carboxamideIC5033.0 [1], 756.0 [2]
3-{[(4-Chlorophenyl)methyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamideIC507.0 [1], 300.0 [2]
3-{[1-(4-Chlorophenyl)ethyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamideIC503.0 [1], 96.0 [2]
3-{[1-(4-Chlorophenyl)propyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamideIC509.0 [1], 70.0 [2]
3-{[(1R)-1-(4-Chlorophenyl)propyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamideIC504.0 [1], 46.0 [2]
3-{[(1S)-1-(4-Chlorophenyl)propyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamideIC5052.0 [1], 978.0 [2]
3-[1-(4-Chlorophenyl)-2-methylpropyl]sulfanyl-5-(methylcarbamoylamino)-1,2-thiazole-4-carboxamideIC5016.0 [1], 290.0 [2]
3-{[1-(4-Chlorophenyl)butyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamideIC5035.0 [1], 600.0 [2]
3-[1-(4-Chlorophenyl)-2,2,2-trifluoroethyl]sulfanyl-5-(methylcarbamoylamino)-1,2-thiazole-4-carboxamideIC50110.0 [1], 2870.0 [2]
3-[(Cyclohexylmethyl)sulfanyl]-5-(pyridin-3-ylamino)-1,2-thiazole-4-carboxamideIC50610.0 [1], 1000.0 [2]
5-(Carbamoylamino)-3-[(5-chloro-2,3-dihydro-1H-inden-1-yl)sulfanyl]-1,2-thiazole-4-carboxamideIC5010.0 [1], 110.0 [2]
3-[(5-Chloro-2,3-dihydro-1H-inden-1-yl)sulfanyl]-5-(methylcarbamoylamino)-1,2-thiazole-4-carboxamideIC508.0 [1], 118.0 [2]
5-(Carbamoylamino)-3-(1,2,3,4-tetrahydronaphthalen-1-ylsulfanyl)-1,2-thiazole-4-carboxamideIC50105.0 [1], 1170.0 [2]
5-[(Methylcarbamoyl)amino]-3-(1,2,3,4-tetrahydronaphthalen-1-ylsulfanyl)-1,2-thiazole-4-carboxamideIC50111.0 [1], 1020.0 [2]
5-(Carbamoylamino)-3-{6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ylsulfanyl}-1,2-thiazole-4-carboxamideIC501.0 [1], 17.0 [2]
6-[(2R)-2-(2,5-Difluorophenyl)pyrrolidin-1-yl]-N-[(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)methyl]pyrido[3,2-d]pyrimidin-4-amineIC501.5 [1], 13.0 [2]
4-(3-Ethoxyphenyl)-1-[2-[4-(trifluoromethoxy)phenoxy]ethyl]pyrrolo[3,2-c]pyridine-2-carboxylic acidIC5059.0 [1], 348.0 [2]
5-Cyano-1-{2-[4-(trifluoromethoxy)phenoxy]ethyl}-1H-indole-2-carboxylic acidIC50118.0 [1], 150.0 [2]
5-(1H-Pyrazol-5-yl)-1-[2-[4-(trifluoromethoxy)phenoxy]ethyl]indole-2-carboxylic acidIC5029.0 [1], 51.0 [2]
1-[2-(4-Chlorophenoxy)ethyl]-4-(3-ethoxyphenyl)pyrrolo[3,2-c]pyridine-2-carboxylic acidIC50200.0 [1], 653.0 [2]
4-(3-Ethoxyphenyl)-1-(2-phenoxyethyl)pyrrolo[3,2-c]pyridine-2-carboxylic acidIC50109.0 [1], 2070.0 [2]
1-[2-[4-(Trifluoromethoxy)phenoxy]ethyl]pyrrolo[3,2-c]pyridine-2-carboxylic acidIC5012300.0 [1], 15750.0 [2]
2-[(4S)-7-(3-Chlorophenyl)-1-oxo-3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-4-yl]-N-[(1S)-1-cyclohexyl-2-(4-methylpiperazin-1-yl)ethyl]acetamideIC5010000.0 [1]
1-Cyclopropyl-1-[3-(1,3-Thiazol-2-Yl)benzyl]-3-[4-(Trifluoromethoxy)phenyl]ureaIC50549.0 [1], 4233.0 [2]
1-Propan-2-yl-1-[[3-(1,3-thiazol-2-yl)phenyl]methyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC5056.0 [1], 132.0 [2]
N-(2,2-Dimethylpropyl)-2-(1-oxo-7-thiophen-3-yl-3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-4-yl)acetamideIC5010000.0 [1]
6-N-[(3-Chlorophenyl)methyl]-4-N-[4-(4-methylpiperazin-1-yl)phenyl]pyrido[3,2-d]pyrimidine-4,6-diamineIC5011.0 [1], 1688.0 [2]
N-(5-Cyclopropyl-2-phenylpyrazol-3-yl)-2-[4-[4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamideIC509.0 [1], 60.0 [2]
Trk Inhibitor C11IC507.0 [1], 9.0 [2]
1-[[3-Methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]-5-(1-methylpyrazol-4-yl)benzimidazol-2-amineIC500.3 [1], 1.0 [2]
3-(4-Chloro-benzylsulfanyl)-5-(pyridin-4-ylamino)-isothiazole-4-carboxylic acid amideIC5045.0 [1], 344.0 [2]
1-[2-(3-Methylphenyl)-5-(trifluoromethyl)pyridin-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC503.0 [1], 30.0 [2]
1-[2-[4-[2-(Ethylamino)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]-3-[2-(4-methylphenyl)-5-(trifluoromethyl)pyridin-3-yl]ureaIC504.0 [1], 90.0 [2]
5-[(2,4-Dichloro-5-pyridin-2-ylbenzoyl)amino]-N-(4-hydroxycyclohexyl)-1-phenylpyrazole-3-carboxamideIC506.93 [1], 7.23 [2]
5-[[2,4-Dichloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-(4-hydroxycyclohexyl)-1-phenylpyrazole-3-carboxamideIC504.03 [1], 4.46 [2]
5-[[2-Chloro-4-fluoro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-(4-hydroxycyclohexyl)-1-phenylpyrazole-3-carboxamideIC509.71 [1], 12.0 [2]
N-(3-Aminocyclobutyl)-5-[(2-chloro-4-fluoro-5-pyridin-2-ylbenzoyl)amino]-1-phenylpyrazole-3-carboxamideIC50104.0 [1], 126.0 [2]
5-[[2-Chloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-[3-(hydroxymethyl)cyclobutyl]-1-phenylpyrazole-3-carboxamideIC5067.6 [1], 82.6 [2]
5-[(2-Chloro-4-fluoro-5-pyridin-2-ylbenzoyl)amino]-N-(3-hydroxycyclobutyl)-1-phenylpyrazole-3-carboxamideIC5025.9 [1], 28.7 [2]
5-[(2-Chloro-4-fluoro-5-pyridin-2-ylbenzoyl)amino]-N-[3-(hydroxymethyl)cyclobutyl]-1-phenylpyrazole-3-carboxamideIC5025.9 [1], 26.3 [2]
5-[(2-Chloro-4-fluoro-5-pyridin-2-ylbenzoyl)amino]-N-(4-hydroxycyclohexyl)-1-phenylpyrazole-3-carboxamideIC5020.9 [1], 22.0 [2]
N-(3-Aminocyclobutyl)-5-[[2-chloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-1-phenylpyrazole-3-carboxamideIC50196.0 [1], 234.0 [2]
N-(4-Aminocyclohexyl)-5-[[2-chloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-1-phenylpyrazole-3-carboxamideIC50114.0 [1], 164.0 [2]
5-[[2,4-Dichloro-5-(5-fluoropyridin-2-yl)benzoyl]amino]-N-(4-hydroxycyclohexyl)-1-phenylpyrazole-3-carboxamideIC5017.4 [1], 22.0 [2]
5-[[2,4-Dichloro-5-(5-fluoropyridin-2-yl)benzoyl]amino]-N-(3-hydroxycyclobutyl)-1-phenylpyrazole-3-carboxamideIC5024.2 [1], 25.2 [2]
5-[[2-Chloro-4-fluoro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-(3-hydroxycyclobutyl)-1-phenylpyrazole-3-carboxamideIC5011.3 [1], 14.2 [2]
5-[[2,4-Dichloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-(3-hydroxycyclobutyl)-1-phenylpyrazole-3-carboxamideIC504.69 [1], 5.83 [2]
5-[(2,4-Dichloro-5-pyridin-2-ylbenzoyl)amino]-N-(3-hydroxycyclobutyl)-1-phenylpyrazole-3-carboxamideIC507.46 [1], 13.1 [2]
N-(3-Aminocyclobutyl)-5-[(2,4-dichloro-5-pyridin-2-ylbenzoyl)amino]-1-phenylpyrazole-3-carboxamideIC5038.1 [1], 46.9 [2]
N-(3-Aminocyclobutyl)-5-[[2-chloro-4-fluoro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-1-phenylpyrazole-3-carboxamideIC5053.1 [1], 81.3 [2]
N-(3-Aminocyclobutyl)-5-[[2,4-dichloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-1-phenylpyrazole-3-carboxamideIC5027.2 [1], 31.5 [2]
N-(3-Aminocyclobutyl)-5-[[2,4-dichloro-5-(5-fluoropyridin-2-yl)benzoyl]amino]-1-phenylpyrazole-3-carboxamideIC50116.0 [1], 142.0 [2]
5-[[2-Chloro-5-(3-fluoropyridin-2-yl)benzoyl]amino]-N-(4-hydroxycyclohexyl)-1-phenylpyrazole-3-carboxamideIC5057.1 [1], 67.1 [2]
1-[2-[4-[2-(2-Oxopiperidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]-3-[5-(trifluoromethyl)-2-[6-(trifluoromethyl)pyridin-3-yl]pyridin-3-yl]ureaIC5093.0 [1], 160.0 [2]
1-[2-[4-[2-(2-Oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]-3-[5-(trifluoromethyl)-2-[6-(trifluoromethyl)pyridin-3-yl]pyridin-3-yl]ureaIC5012.0 [1], 40.0 [2]
1-[5-(1,1-Difluoroethyl)-2-(2-methylphenyl)pyrazol-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC5018.0 [1], 60.0 [2]
1-[2-[4-[2-(Ethylamino)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]-3-[2-phenoxy-5-(trifluoromethyl)pyridin-3-yl]ureaIC5010.0 [1], 120.0 [2]
1-[2-(2-Methylphenyl)-5-(trifluoromethyl)pyrazol-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC5011.0 [1], 50.0 [2]
1-(5-Cyclopropyl-2-phenylpyrazol-3-yl)-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC5030.0 [1], 33.0 [2]
1-[2-(3,4-Dimethylphenyl)-5-(trifluoromethyl)pyridin-3-yl]-3-[2-[4-[2-(2-oxoazepan-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC5070.0 [1], 190.0 [2]
Methyl 3-[3-tert-butyl-5-[[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]carbamoylamino]pyrazol-1-yl]benzoateIC5010.0 [1], 130.0 [2]
1-[2-Chloro-5-(trifluoromethyl)phenyl]-3-[2-[4-[2-(propylamino)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC502.0 [1], 20.0 [2]
1-[2-(3,4-Dimethylphenyl)-5-(trifluoromethyl)pyridin-3-yl]-3-[6-[4-[2-(ethylamino)-1,3-thiazol-5-yl]phenoxy]pyridin-3-yl]ureaIC506.0 [1], 180.0 [2]
1-[5-Tert-butyl-2-(3,4-dimethylphenyl)pyrazol-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC502.0 [1], 80.0 [2]
N-[4-[3-Tert-butyl-5-[[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]carbamoylamino]pyrazol-1-yl]phenyl]acetamideIC5014.0 [1], 80.0 [2]
1-[5-Tert-butyl-2-(1-methylindazol-5-yl)pyrazol-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC502.0 [1], 30.0 [2]
1-[5-Tert-butyl-2-(4-sulfamoylphenyl)pyrazol-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC5032.0 [1], 50.0 [2]
1-[2-[4-[2-(2-Oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]-3-[2-phenyl-5-(trifluoromethyl)pyridin-3-yl]ureaIC504.0 [1], 40.0 [2]
1-[5-Tert-butyl-2-(2,3-dihydro-1-benzofuran-5-yl)pyrazol-3-yl]-3-[2-[4-[2-(2-oxopyrrolidin-1-yl)-1,3-thiazol-5-yl]phenoxy]pyrimidin-5-yl]ureaIC504.0 [1], 20.0 [2]
AmitriptylineIC5060000.0 [1]
Staurosporine HClIC501.41 [1]
K252aIC5013.0 [1]
BosutinibIC5022.0 [1]
PictilisibIC502850.0 [1]
CeritinibIC502727.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Nerve growth factor receptor Trk-A Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Nov. 2024, https://www.aatbio.com/data-sets/nerve-growth-factor-receptor-trk-a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 20). Quest Database™ Nerve growth factor receptor Trk-A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/nerve-growth-factor-receptor-trk-a-inhibitors-ic50-ki.
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