Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.22 extracted from

  • Traquandi, G.; Ciomei, M.; Ballinari, D.; Casale, E.; Colombo, N.; Croci, V.; Fiorentini, F.; Isacchi, A.; Longo, A.; Mercurio, C.; Panzeri, A.; Pastori, W.; Pevarello, P.; Volpi, D.; Roussel, P.; Vulpetti, A.; Brasca, M.G.
    Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors (2010), J. Med. Chem., 53, 2171-2187.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
cyclin A activates Cdk2 Homo sapiens

Inhibitors

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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-2780 cell
-
Homo sapiens
-
ovarian carcinoma cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
CDK
-
Homo sapiens
CDK2
-
Homo sapiens

IC50 Value

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