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Literature summary for 2.7.11.13 extracted from

  • Li, H.; Hong, Y.; Nukui, S.; Lou, J.; Johnson, S.; Scales, S.; Botrous, I.; Tompkins, E.; Yin, C.; Zhou, R.; He, M.; Jensen, J.; Bouzida, D.; Alton, G.; Lafontaine, J.; Grant, S.
    Identification of novel pyrrolopyrazoles as protein kinase C beta II inhibitors (2011), Bioorg. Med. Chem. Lett., 21, 584-587.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
N-(5'-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-4',5'-dihydro-1'H-spiro[cyclopropane-1,6'-pyrrolo[3,4-c]pyrazol]-3'-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-phenoxybenzamide
-
Homo sapiens
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
Homo sapiens
N-(5-([(3S,7S,8aS)-7-fluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(5-([(3S,8aS)-3-ethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(5-([(3S,8aS)-7,7-difluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(5-([(8aS)-3,3-dimethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(6,6-dimethyl-5-([(3R,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide 0.001 mM, 13% inhibition Homo sapiens
N-(6,6-dimethyl-5-([(3R,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide 0.001 mM, 24% inhibition Homo sapiens
N-(6,6-dimethyl-5-([(3S,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(6,6-dimethyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(6,6-dimethyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
Homo sapiens
N-(6-ethyl-6-methyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
Homo sapiens
N-[5-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]benzamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
PKC beta II
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000029
-
N-(6,6-dimethyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000046
-
N-(5-([(3S,8aS)-3-ethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000062
-
N-(6-ethyl-6-methyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000092
-
N-(6,6-dimethyl-5-([(3S,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000109
-
N-(5-([(3S,7S,8aS)-7-fluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000125
-
N-(5-([(8aS)-3,3-dimethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000131
-
N-[5-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]benzamide pH and temperature not specified in the publication Homo sapiens
0.000189
-
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.000338
-
N-(5'-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-4',5'-dihydro-1'H-spiro[cyclopropane-1,6'-pyrrolo[3,4-c]pyrazol]-3'-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000541
-
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-phenoxybenzamide pH and temperature not specified in the publication Homo sapiens
0.000541
-
N-(6,6-dimethyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.01
-
N-(5-([(3S,8aS)-7,7-difluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens