| Reaction Details |
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 | Report a problem with these data |
| Target | 3-phosphoinositide-dependent protein kinase 1 |
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| Ligand | BDBM50321582 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_799415 (CHEMBL1942167) |
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| IC50 | 85±n/a nM |
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| Citation |  Murphy, ST; Alton, G; Bailey, S; Baxi, SM; Burke, BJ; Chappie, TA; Ermolieff, J; Ferre, R; Greasley, S; Hickey, M; Humphrey, J; Kablaoui, N; Kath, J; Kazmirski, S; Kraus, M; Kupchinsky, S; Li, J; Lingardo, L; Marx, MA; Richter, D; Tanis, SP; Tran, K; Vernier, W; Xie, Z; Yin, MJ; Yu, XH Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1). J Med Chem54:8490-500 (2011) [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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| BDBM50321582 |
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| n/a |
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| Name | BDBM50321582 |
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| Synonyms: | 1-(3-aminopropyl)-8-(3-(2-(dimethylamino)-2-oxoethyl)phenylamino)-N-((2-methylpyridin-4-yl)methyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1172241 |
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| Type | Small organic molecule |
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| Emp. Form. | C30H35N9O2 |
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| Mol. Mass. | 553.658 |
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| SMILES | CN(C)C(=O)Cc1cccc(Nc2ncc3CCc4c(nn(CCCN)c4-c3n2)C(=O)NCc2ccnc(C)c2)c1 |
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| Structure | 
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