| Reaction Details |
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 | Report a problem with these data |
| Target | 3-phosphoinositide-dependent protein kinase 1 |
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| Ligand | BDBM138348 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1510637 (CHEMBL3608088) |
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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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| 3-phosphoinositide-dependent protein kinase 1 |
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| Name: | 3-phosphoinositide-dependent protein kinase 1 |
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| Synonyms: | 3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide dependent protein kinase-1 | 3-phosphoinositide-dependent protein kinase 1 | 3-phosphoinositide-dependent protein kinase 1 (PDK) | 3-phosphoinositide-dependent protein kinase 1 (PDK-1) | 3-phosphoinositide-dependent protein kinase 1 (PDK1)(Δ1-50) | Isoform 2 of 3-phosphoinositide-dependent protein kinase 1 | PDK1 | PDPK1 | PDPK1_HUMAN | Phosphoinositide-dependent protein kinase 1 (PDK1) | Pyruvate dehydrogenase kinase isoenzyme 1 (PDK1) | hPDK1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 63157.65 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O15530 |
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| Residue: | 556 |
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| Sequence: | MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRP
GAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIK
ENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDET
CTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARAN
SFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYD
FPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTA
YLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLD
SNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTE
GPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQ
EVWRQRYQSHPDAAVQ
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| BDBM138348 |
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| n/a |
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| Name | BDBM138348 |
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| Synonyms: | US8877944, 99 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H24F3N3O2 |
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| Mol. Mass. | 395.4187 |
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| SMILES | NC(=O)c1cc(F)cc2CN(C3CCN(CC3)C3CCC(F)(F)CC3)C(=O)c12 |
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| Structure | 
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