Reaction Details |
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Target | Cyclin-A2/Cyclin-dependent kinase 2 |
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Ligand | BDBM138348 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1510605 (CHEMBL3607953) |
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IC50 | >10000±n/a nM |
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Citation | Papeo, G; Posteri, H; Borghi, D; Busel, AA; Caprera, F; Casale, E; Ciomei, M; Cirla, A; Corti, E; D'Anello, M; Fasolini, M; Forte, B; Galvani, A; Isacchi, A; Khvat, A; Krasavin, MY; Lupi, R; Orsini, P; Perego, R; Pesenti, E; Pezzetta, D; Rainoldi, S; Riccardi-Sirtori, F; Scolaro, A; Sola, F; Zuccotto, F; Felder, ER; Donati, D; Montagnoli, A Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. J Med Chem58:6875-98 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-A2/Cyclin-dependent kinase 2 |
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Name: | Cyclin-A2/Cyclin-dependent kinase 2 |
Synonyms: | CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | CDK2/Cyclin A2 | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-Dependent Kinase 2 (CDK2A) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cyclin-dependent kinase 2 |
Synonyms: | CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase |
Type: | Enzyme Subunit |
Mol. Mass.: | 33938.17 |
Organism: | Homo sapiens (Human) |
Description: | P24941 |
Residue: | 298 |
Sequence: | MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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Component 2 |
Name: | Cyclin-A2 |
Synonyms: | CCN1 | CCNA | CCNA1 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A |
Type: | Enzyme Subunit |
Mol. Mass.: | 48550.19 |
Organism: | Homo sapiens (Human) |
Description: | P20248 |
Residue: | 432 |
Sequence: | MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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BDBM138348 |
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n/a |
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Name | BDBM138348 |
Synonyms: | US8877944, 99 |
Type | Small organic molecule |
Emp. Form. | C20H24F3N3O2 |
Mol. Mass. | 395.4187 |
SMILES | NC(=O)c1cc(F)cc2CN(C3CCN(CC3)C3CCC(F)(F)CC3)C(=O)c12 |
Structure |
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