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Epithelial discoidin domain-containing receptor 1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
ImatinibIC5043.0 [1], 90.0 [2], 337.0 [3], 31000.0 [4]
NilotinibIC503.7 [1], 32.6 [2], 43.0 [3], 100.0 [4]
DasatinibIC500.5 [1], 4.8 [2]
Ddr1-IN-2IC506.81 [1], 9.7 [2]
3-[[2-[3-(Morpholin-4-ylmethyl)phenyl]thieno[3,2-b]pyridin-7-yl]amino]phenolIC50164.0 [1]
Ddr1-IN-1IC5086.0 [1], 105.0 [2]
4-[(4-Ethylpiperazin-1-yl)methyl]-N-[3-[(4-methoxy-1H-pyrrolo[2,3-b]pyridin-5-yl)methylamino]-4-methylphenyl]-3-(trifluoromethyl)benzamideIC509.0 [1], 47.0 [2]
BemcentinibIC5020.0 [1]
Dual DDR1 and DDR2 inhibitor 5nIC509.4 [1]
1-(2-Chlorophenyl)-3-(pyridin-3-ylmethyl)ureaIC50100000.0 [1]
Chmfl-bmx-078IC50265.0 [1]
1-[5-Tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-[2-(pyridin-4-ylmethoxy)ethyl]-1,3-thiazol-2-yl]ureaIC5068.0 [1]
Chmfl-abl-053IC50292.0 [1]
Chmfl-kit-110IC50126.0 [1]
Ripk1-IN-7IC5035.0 [1]
[6-Chloro-4-methyl-3-[[3-(methylsulfamoylamino)phenyl]methyl]-2-oxochromen-7-yl] N,N-dimethylcarbamateIC5050000.0 [1]
5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamideIC5010000.0 [1]
N-(7-Methoxyquinolin-6-yl)thieno[3,2-d]pyrimidine-7-carboxamideIC5050000.0 [1]
1-[1-(3-Aminophenyl)-3-Tert-Butyl-1h-Pyrazol-5-Yl]-3-[4-(Quinazolin-4-Ylamino)phenyl]ureaIC5039.0 [1]
6-(2,4-Difluorophenyl)sulfonyl-2-(1H-indol-5-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-oneIC5010000.0 [1]
CID 71624791IC502.29 [1]
1-[2-(3-Aminophenyl)-5-tert-butylpyrazol-3-yl]-3-[3-(quinazolin-4-ylamino)phenyl]ureaIC50235.0 [1]
N-[3-[(Phenylcarbamoylamino)methyl]phenyl]imidazo[1,2-a]pyridine-3-carboxamideIC50150.0 [1]
3-[(4-Methylpiperazin-1-yl)methyl]-N-[(4R)-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinolin-7-yl]-5-(trifluoromethyl)benzamideIC5075.7 [1]
4-(Methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamideIC50212.0 [1]
CID 129318936IC502462.0 [1]
4-Methyl-2-pyrimidin-5-yl-N-[3-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50191.0 [1]
N-[3-[(Dimethylamino)methyl]-5-(trifluoromethyl)phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50254.0 [1]
4-Methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5038.3 [1]
4-Methyl-N-[3-[2-(4-methylpiperazin-1-yl)ethyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5080.7 [1]
4,4-Dimethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-1,3-dihydroisoquinoline-7-carboxamideIC50223.0 [1]
N-[3-Cyclopropyl-5-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5089.0 [1]
N-[3-Cyclohexyl-5-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50123.0 [1]
N-[3-[(4-Cyclohexylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5079.9 [1]
N-[3-[(4-Ethylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5071.1 [1]
N-[3-Ethyl-5-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5050.5 [1]
4-Methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-propan-2-ylphenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5049.9 [1]
N-[3-Tert-butyl-5-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5066.6 [1]
3-[(4-Methylpiperazin-1-yl)methyl]-N-[(4S)-4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinolin-7-yl]-5-(trifluoromethyl)benzamideIC50614.0 [1]
4-Methyl-2-pyrimidin-5-yl-N-[3-(thiomorpholin-4-ylmethyl)-5-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50209.0 [1]
4-Methyl-N-[3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50132.0 [1]
4-Methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5019.9 [1]
4-Methyl-2-pyrimidin-5-yl-N-[3-(pyrrolidin-1-ylmethyl)-5-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50222.0 [1]
4-Methyl-N-[3-[(4-methyl-1,4-diazepan-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5025.6 [1]
3-Methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50545.0 [1]
4-Methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-phenylphenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5044.6 [1]
4-Methyl-N-[3-(piperidin-1-ylmethyl)-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50167.0 [1]
1-[4-[4-Amino-3-[4-(2-morpholin-4-ylethoxy)phenyl]pyrazolo[3,4-d]pyrimidin-1-yl]phenyl]-3-(5-tert-butyl-1,2-oxazol-3-yl)ureaIC5063.0 [1]
Chmfl-abl/kit-155IC50116.0 [1]
4-Methyl-N-[3-(morpholin-4-ylmethyl)-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50193.0 [1]
5,5-Dimethyl-8-[[4-(2,2,2-trifluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-1H-4,1-benzoxazepin-2-oneIC5010000.0 [1]
(4S)-4-Methyl-N-[3-[(4-methyl-1,4-diazepan-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC50167.0 [1]
4-Methyl-N-[2-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5010000.0 [1]
(E)-4-(Dimethylamino)-N-[2-methyl-5-[9-(1-methylpyrazol-4-yl)-2-oxobenzo[h]quinolin-1-yl]phenyl]but-2-enamideIC505020.0 [1]
4-Methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5010000.0 [1]
4-Ethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyridin-6-ylethynyl)benzamideIC5013.1 [1]
N-[3-[(4-Methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-(pyrimidin-5-ylmethyl)-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5010000.0 [1]
N-[3-[(4-Methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-4-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC5010000.0 [1]
1-[3-[(4-Methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-3-(4-methyl-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinolin-7-yl)ureaIC5010000.0 [1]
(4R)-4-Methyl-N-[3-[(4-methyl-1,4-diazepan-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1H-isoquinoline-7-carboxamideIC506.6 [1]
4-Ethyl-3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC503.2 [1]
4-Ethyl-3-[2-(furan-3-yl)ethynyl]-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC50151.0 [1]
4-Ethyl-3-(2-imidazo[1,2-a]pyridin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC506.2 [1]
3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-propan-2-ylbenzamideIC5011.4 [1]
4-Ethyl-3-[2-[2-(methylamino)pyrimidin-5-yl]ethynyl]-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC505.0 [1]
3-(2-Imidazo[1,2-a]pyridin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-propan-2-ylbenzamideIC5012.5 [1]
4-Ethyl-3-[2-(furan-2-yl)ethynyl]-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC501200.0 [1]
3-[2-(2,3-Dimethylimidazol-4-yl)ethynyl]-4-ethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC507.9 [1]
4-Ethyl-3-[2-(3-methylimidazol-4-yl)ethynyl]-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC5016.0 [1]
3-[2-[2-(Dimethylamino)pyrimidin-5-yl]ethynyl]-4-ethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC50614.0 [1]
4-Ethyl-3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC503.9 [1]
4-Tert-butyl-3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC50380.0 [1]
4-Ethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrimidin-5-ylethynyl)benzamideIC508.4 [1]
3-[2-(2-Aminopyrimidin-5-yl)ethynyl]-4-ethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC503.9 [1]
1-(Cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]pyrazolo[3,4-d]pyrimidin-6-amineIC50100.0 [1]
1-(Cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-6-amineIC5035.0 [1]
4-Cyclopropyl-3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC5012.6 [1]
4-Ethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-thiophen-3-ylethynyl)benzamideIC50695.0 [1]
3-(2-Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]benzamideIC502.4 [1]
3-[(E)-2-(4-Chlorophenyl)ethenyl]-N-[(2R)-2,3-dihydroxypropyl]-4-methoxybenzamideIC5050000.0 [1]
3-[(E)-2-(4-Chlorophenyl)ethenyl]-N-[(2S)-2,3-dihydroxypropyl]-4-methoxybenzamideIC5050000.0 [1]
4-Methyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC508.93 [1]
N-[3-[(4-Methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC507.02 [1]
4-Methyl-N-propan-2-yl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5039.63 [1]
N-Butyl-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5065.14 [1]
4-Methyl-N-(2-methylpropyl)-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC501000.0 [1]
N-Cyclohexyl-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5029.15 [1]
N-Cyclopentyl-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5039.82 [1]
4-Methyl-N-phenyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5038.9 [1]
4-Methyl-N-(2-methylphenyl)-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC501000.0 [1]
4-Methyl-N-(3-methylphenyl)-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC505.96 [1]
4-Methyl-N-(4-methylphenyl)-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5047.75 [1]
N-(2-Chlorophenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC501000.0 [1]
N-(4-Chlorophenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC501000.0 [1]
N-(2-Methoxyphenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC50470.0 [1]
N-(3-Methoxyphenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC504.04 [1]
N-(4-Methoxyphenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5022.36 [1]
N-(3-Bromophenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5016.64 [1]
N-(3-Iodophenyl)-4-methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamideIC5019.75 [1]
4-Methyl-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-N-[3-(trifluoromethyl)phenyl]benzamideIC506.14 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Epithelial discoidin domain-containing receptor 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/epithelial-discoidin-domain-containing-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ Epithelial discoidin domain-containing receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/epithelial-discoidin-domain-containing-receptor-1-inhibitors-ic50-ki.
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