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Serine/threonine-protein kinase PAK 1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
PF-03758309IC5013.7 [1], 14.0 [2]
PF-03758309Ki15.0 [1], 36.0 [2], 39.0 [3]
8-Chloro-3-fluoro-11-methyl-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzodiazepineIC50900.0 [1], 1000.0 [2], 6000.0 [3], 9000.0 [4], 25000.0 [5]
CID 70934541IC502.8 [1], 7.7 [2], 10.0 [3], 88.0 [4]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-oneIC5010.0 [1], 222.0 [2]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-oneKi22.0 [1], 23.0 [2]
1-({1-(2-Aminopyrimidin-4-Yl)-2-[(2-Methoxyethyl)amino]-1h-Benzimidazol-6-Yl}ethynyl)cyclohexanolIC502000.0 [1], 5420.0 [2]
1-({1-(2-Aminopyrimidin-4-Yl)-2-[(2-Methoxyethyl)amino]-1h-Benzimidazol-6-Yl}ethynyl)cyclohexanolKi2900.0 [1]
8-[(5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneIC5069.0 [1]
8-[(5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneKi3.7 [1]
2-[[N-[2-[3-Ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-5-(hydroxymethyl)-2-methylanilino]methyl]benzonitrileIC500.33 [1], 1.0 [2], 59.0 [3]
2-N-[(4-Chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-N-methylpyrimidine-2,4-diamineIC50110.0 [1]
2-N-[(4-Chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-N-methylpyrimidine-2,4-diamineKi4.0 [1], 5.0 [2]
4-N-(5-Cyclopropyl-1H-pyrazol-3-yl)-2-N-[(1S)-1-(1H-indol-5-yl)ethyl]pyrimidine-2,4-diamineIC50120.0 [1]
4-N-(5-Cyclopropyl-1H-pyrazol-3-yl)-2-N-[(1S)-1-(1H-indol-5-yl)ethyl]pyrimidine-2,4-diamineKi31.0 [1]
[3-[[2-[3-Ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-methylamino]-4-methylphenyl]methanolIC502.1 [1], 490.0 [2], 540.0 [3]
N~2~-[(trans-4-Aminocyclohexyl)methyl]-N~4~-(3-Cyclopropyl-1h-Pyrazol-5-Yl)pyrimidine-2,4-DiamineIC502200.0 [1]
N~2~-[(trans-4-Aminocyclohexyl)methyl]-N~4~-(3-Cyclopropyl-1h-Pyrazol-5-Yl)pyrimidine-2,4-DiamineKi21.0 [1], 26.0 [2]
Bis(2-hydroxy-1-naphthyl) disulfideIC501000.0 [1], 2500.0 [2]
CID 68060125IC508.3 [1], 10.0 [2]
[4-Methyl-3-[methyl-[2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]amino]phenyl]methanolIC50100.0 [1], 3100.0 [2]
4-N-(5-Cyclopropyl-1H-pyrazol-3-yl)-2-N-(1H-indol-5-ylmethyl)pyrimidine-2,4-diamineKi27.0 [1], 70.0 [2]
4-[1-(4-Amino-1,3,5-Triazin-2-Yl)-2-(Ethylamino)-1h-Benzimidazol-6-Yl]-2-Methylbut-3-Yn-2-OlIC509600.0 [1]
4-[1-(4-Amino-1,3,5-Triazin-2-Yl)-2-(Ethylamino)-1h-Benzimidazol-6-Yl]-2-Methylbut-3-Yn-2-OlKi4500.0 [1]
CID 73348907IC5064.1 [1]
CID 73348907Ki36.8 [1]
8-[(5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneIC50148.0 [1]
8-[(5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneKi8.0 [1]
8-[(4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneIC50341.0 [1]
8-[(4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneKi7.4 [1]
6-[2-Chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(methylamino)-8-[[5-(methylamino)-1,3-dioxan-2-yl]methyl]pyrido[2,3-d]pyrimidin-7-oneIC5057.0 [1]
6-[2-Chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(methylamino)-8-[[5-(methylamino)-1,3-dioxan-2-yl]methyl]pyrido[2,3-d]pyrimidin-7-oneKi1.9 [1]
6-[2-Chloro-4-(6-methylpyridin-2-yl)phenyl]-8-(5,9-dioxa-2-azaspiro[3.5]nonan-7-ylmethyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneIC5073.0 [1]
6-[2-Chloro-4-(6-methylpyridin-2-yl)phenyl]-8-(5,9-dioxa-2-azaspiro[3.5]nonan-7-ylmethyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneKi4.3 [1]
2-N-[(4-Chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-N-ethylpyrimidine-2,4-diamineIC5085.0 [1]
2-N-[(4-Chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-N-ethylpyrimidine-2,4-diamineKi5.0 [1]
(3R)-3-[3-[[2-[(4-Chloro-1H-benzimidazol-5-yl)methyl-methylamino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methylpyrrolidin-2-oneIC507800.0 [1]
(3R)-3-[3-[[2-[(4-Chloro-1H-benzimidazol-5-yl)methyl-methylamino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methylpyrrolidin-2-oneKi18.0 [1]
(3R)-3-[3-[[2-[(4-Aminocyclohexyl)methyl-methylamino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methylpyrrolidin-2-oneIC5010000.0 [1]
(3R)-3-[3-[[2-[(4-Aminocyclohexyl)methyl-methylamino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methylpyrrolidin-2-oneKi37.0 [1]
(3R)-3-[3-[[2-[(4-Aminocyclohexyl)methyl-ethylamino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methylpyrrolidin-2-oneIC5010000.0 [1]
(3R)-3-[3-[[2-[(4-Aminocyclohexyl)methyl-ethylamino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methylpyrrolidin-2-oneKi49.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(3-hydroxypropyl)pyrido[2,3-d]pyrimidin-7-oneIC50980.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(3-hydroxypropyl)pyrido[2,3-d]pyrimidin-7-oneKi64.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-[(2-oxopiperidin-4-yl)methyl]pyrido[2,3-d]pyrimidin-7-oneIC50813.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-[(2-oxopiperidin-4-yl)methyl]pyrido[2,3-d]pyrimidin-7-oneKi66.0 [1]
6-[2-Chloro-4-(6-methylpyridin-2-yl)phenyl]-8-[[(4S)-3,3-difluoropiperidin-4-yl]methyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneIC5053.0 [1]
6-[2-Chloro-4-(6-methylpyridin-2-yl)phenyl]-8-[[(4S)-3,3-difluoropiperidin-4-yl]methyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-oneKi7.9 [1]
[5-[[5-Fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanolIC503.0 [1], 220.0 [2]
[5-[[2-[3-Ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanolIC500.45 [1], 200.0 [2]
[3-[[5-Fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]phenyl]methanolIC5045.0 [1], 14000.0 [2]
[5-[[5-Fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]-2-methylphenyl]methanolIC5019.0 [1], 420.0 [2]
[5-[[2-(3-Ethylsulfonyl-5-morpholin-4-ylanilino)-5-fluoropyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanolIC502.8 [1], 270.0 [2]
[3-[Benzyl-[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]amino]-4-methylphenyl]methanolIC501.5 [1], 230.0 [2]
[3-[Ethyl-[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]amino]-4-methylphenyl]methanolIC502.0 [1], 530.0 [2]
[3-[[2-[3-Ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-[(2-fluorophenyl)methyl]amino]-4-methylphenyl]methanolIC500.35 [1], 130.0 [2]
[5-[[5-Fluoro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanolIC5033.0 [1], 2100.0 [2]
[5-[[2-[3-Ethylsulfonyl-4-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]anilino]-5-fluoropyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanolIC500.58 [1], 110.0 [2]
[3-[[5-Fluoro-2-[4-(4-methylpiperazin-1-yl)-3-methylsulfonylanilino]pyrimidin-4-yl]-methylamino]-4-methylphenyl]methanolIC508.7 [1], 810.0 [2]
5-Fluoro-4-N-[5-(methoxymethyl)-2-methylphenyl]-4-N-methyl-2-N-(3-methylsulfonyl-5-morpholin-4-ylphenyl)pyrimidine-2,4-diamineIC50189.0 [1], 3300.0 [2]
[3-[[5-Fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]-4-methylphenyl]methanolIC5014.0 [1], 860.0 [2]
[4-Chloro-3-[[5-fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]phenyl]methanolIC509.6 [1], 480.0 [2]
2,8-Difluoro-11-(4-Methylpiperazin-1-Yl)-5h-Dibenzo[b,E][1,4]diazepineIC5012000.0 [1], 54000.0 [2]
4-N-(5-Cyclobutyl-1H-pyrazol-3-yl)-2-N-[(1S)-1-(1H-indol-5-yl)ethyl]pyrimidine-2,4-diamineIC50133.0 [1]
4-N-(5-Cyclobutyl-1H-pyrazol-3-yl)-2-N-[(1S)-1-(1H-indol-5-yl)ethyl]pyrimidine-2,4-diamineKi6.75 [1]
2-N-[(1S)-1-(3H-Benzimidazol-5-yl)ethyl]-4-N-[5-(2,2-difluorocyclopropyl)-1H-pyrazol-3-yl]pyrimidine-2,4-diamineIC50244.0 [1]
2-N-[(1S)-1-(3H-Benzimidazol-5-yl)ethyl]-4-N-[5-(2,2-difluorocyclopropyl)-1H-pyrazol-3-yl]pyrimidine-2,4-diamineKi5.13 [1]
2-[[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]-[(6-fluoro-1H-indazol-4-yl)methyl]amino]propan-1-olIC5070.8 [1]
2-[[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]-[(6-fluoro-1H-indazol-4-yl)methyl]amino]propan-1-olKi4.2 [1]
2-N-[(1S)-1-(3H-Benzimidazol-5-yl)ethyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamineIC50281.0 [1]
2-N-[(1S)-1-(3H-Benzimidazol-5-yl)ethyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamineKi12.0 [1]
2-N-[(4-Chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamineIC50362.0 [1]
2-N-[(4-Chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamineKi5.0 [1]
8-[(4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneIC50124.0 [1]
8-[(4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneKi1.9 [1]
8-(4-Aminobutyl)-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneIC50147.0 [1]
8-(4-Aminobutyl)-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneKi6.1 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(piperidin-4-ylmethyl)pyrido[2,3-d]pyrimidin-7-oneIC50145.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(piperidin-4-ylmethyl)pyrido[2,3-d]pyrimidin-7-oneKi6.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)-8-[[(2R)-morpholin-2-yl]methyl]pyrido[2,3-d]pyrimidin-7-oneIC50399.0 [1]
6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)-8-[[(2R)-morpholin-2-yl]methyl]pyrido[2,3-d]pyrimidin-7-oneKi19.0 [1]
8-[(4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneIC5045.0 [1]
8-[(4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-oneKi2.1 [1]
(2-Chlorophenyl)-[5-(2-methyl-3,4-dihydro-1H-isoquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]methanoneIC501.0 [1], 140.0 [2]
(2-Chlorophenyl)-[5-(1-piperidin-4-ylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]methanoneIC5018.0 [1], 870.0 [2]
(2-Chlorophenyl)-[5-(2-methyl-1,3-dihydroisoindol-5-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]methanoneIC5033.0 [1], 1100.0 [2]
(2-Chlorophenyl)-[5-(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]methanoneIC504.5 [1], 650.0 [2]
1-[6-[3-(2-Chlorobenzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-3,4-dihydro-1H-isoquinolin-2-yl]ethanoneIC50270.0 [1], 1300.0 [2]
5-[2-Chloro-4-(1,3-thiazol-5-yl)phenyl]-3-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-oneIC502.8 [1], 88.0 [2]
CurcuminIC5016000.0 [1]
StaurosporineIC500.3 [1]
ResveratrolIC5015000.0 [1]
KetorolacIC5036000.0 [1]
Sepantronium bromideIC50500.0 [1]
Artepillin CIC5025000.0 [1]
Azd-1152hqpaKi10000.0 [1]
1-(3-Chloro-2,6-dihydroxy-4-methoxyphenyl)-1-hexanoneIC502500.0 [1]
JNK Inhibitor VIIIKi9700.0 [1]
6-Morpholin-4-Yl-9h-PurineIC5018000.0 [1]
N-Cyclopentyl-9H-purin-6-amineIC5018000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Serine/threonine-protein kinase PAK 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/serine-threonine-protein-kinase-pak-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Serine/threonine-protein kinase PAK 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serine-threonine-protein-kinase-pak-1-inhibitors-ic50-ki.
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