Activating Compound | Comment | Organism | Structure |
---|---|---|---|
cyclin A | activates Cdk2 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(R)-roscovitine | - |
Homo sapiens | |
1-(1-acetylpiperidin-4-yl)-8-(cyclopentylamino)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-benzyl-8-(cyclopentylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[(pyridin-2-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[(pyridin-3-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[(pyridin-4-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[1-(phenylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[2-(morpholin-4-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[2-(piperidin-1-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[3-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[4-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
1-methyl-8-[[4-(methylsulfonyl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(benzylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclohexylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclohexylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-(2-hydroxyethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-(4-methoxyphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-(4-sulfamoylphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-(pyridin-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-1-phenyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-N-hydroxy-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-N-methyl-1-(1-methylpiperidin-4-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-N-[1-(dimethylamino)propan-2-yl]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-(cyclopentylamino)-N-[2-(dimethylamino)ethyl]-N-1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-amino-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(1-acetylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(1-ethylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(2-hydroxyethyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(3-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(4-bromobenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[(4-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
8-[[4-(acetylamino)benzyl]amino]-1-methyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
BMS-387032 | - |
Homo sapiens | |
ethyl 4-[[1-methyl-3-(methylcarbamoyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl]amino]piperidine-1-carboxylate | - |
Homo sapiens | |
additional information | evaluation of series of pyrazolo[4,3-h]quinazoline-3-carboxamides as inhibitors using diverse protein kinases, the compounds are active against CDK2/cyclin A, overview | Homo sapiens | |
N-1-dimethyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
N-1-dimethyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
N-1-dimethyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
N-1-dimethyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
N-benzyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
N-cyclohexyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | - |
Homo sapiens | |
PHA-848125 | - |
Homo sapiens | |
[8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-3-yl](4-methylpiperazin-1-yl)methanone | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
A-2780 cell | - |
Homo sapiens | - |
ovarian carcinoma cell | - |
Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
CDK | - |
Homo sapiens |
CDK2 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000001 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000001 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000002 | - |
pH 7.5, 30°C | Homo sapiens | N-1-dimethyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000002 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000002 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(1-acetylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000003 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000004 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclohexylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide | |
0.000004 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[1-(phenylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000005 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000005 | - |
pH 7.5, 30°C | Homo sapiens | N-1-dimethyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000005 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-(4-sulfamoylphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000006 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000006 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-(4-methoxyphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000007 | - |
pH 7.5, 30°C | Homo sapiens | 1-(1-acetylpiperidin-4-yl)-8-(cyclopentylamino)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000008 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-(2-hydroxyethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000012 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000013 | - |
pH 7.5, 30°C | Homo sapiens | 8-[[4-(acetylamino)benzyl]amino]-1-methyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000017 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[4-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000019 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(2-hydroxyethyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | |
0.00002 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-phenyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide | |
0.000021 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[(pyridin-4-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000021 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[(pyridin-3-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000023 | - |
pH 7.5, 30°C | Homo sapiens | 1-benzyl-8-(cyclopentylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide | |
0.000025 | - |
pH 7.5, 30°C | Homo sapiens | N-1-dimethyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000032 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000038 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[4-(methylsulfonyl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000039 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclohexylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | |
0.000051 | - |
pH 7.5, 30°C | Homo sapiens | 8-(benzylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000052 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-1-(pyridin-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000058 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(4-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000059 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-N-methyl-1-(1-methylpiperidin-4-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000066 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(3-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000081 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(4-bromobenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | |
0.000087 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[(pyridin-2-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000097 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | |
0.000104 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[3-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000149 | - |
pH 7.5, 30°C | Homo sapiens | 8-[(1-ethylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000175 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-N-hydroxy-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000209 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[2-(morpholin-4-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000296 | - |
pH 7.5, 30°C | Homo sapiens | N-cyclohexyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.000351 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.001122 | - |
pH 7.5, 30°C | Homo sapiens | N-1-dimethyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.001372 | - |
pH 7.5, 30°C | Homo sapiens | N-benzyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.00176 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-N-[1-(dimethylamino)propan-2-yl]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.00249 | - |
pH 7.5, 30°C | Homo sapiens | 1-methyl-8-[[2-(piperidin-1-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.004585 | - |
pH 7.5, 30°C | Homo sapiens | N-1-dimethyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | 8-amino-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | 8-(cyclopentylamino)-N-[2-(dimethylamino)ethyl]-N-1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | [8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-3-yl](4-methylpiperazin-1-yl)methanone |