Reaction Details |
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Target | Cytochrome P450 3A4 |
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Ligand | BDBM50078374 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1568322 (CHEMBL3788756) |
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IC50 | >50000±n/a nM |
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Citation | Boezio, AA; Copeland, KW; Rex, K; K Albrecht, B; Bauer, D; Bellon, SF; Boezio, C; Broome, MA; Choquette, D; Coxon, A; Dussault, I; Hirai, S; Lewis, R; Lin, MH; Lohman, J; Liu, J; Peterson, EA; Potashman, M; Shimanovich, R; Teffera, Y; Whittington, DA; Vaida, KR; Harmange, JC Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity. J Med Chem59:2328-42 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cytochrome P450 3A4 |
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Name: | Cytochrome P450 3A4 |
Synonyms: | Albendazole monooxygenase | Albendazole sulfoxidase | CP3A4_HUMAN | CYP3A3 | CYP3A4 | CYPIIIA3 | CYPIIIA4 | Cytochrome P450 3A3 | Cytochrome P450 3A4 (CYP3A4) | Cytochrome P450 HLp | Nifedipine oxidase | Quinine 3-monooxygenase | Taurochenodeoxycholate 6-alpha-hydroxylase |
Type: | Enzyme |
Mol. Mass.: | 57349.57 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 503 |
Sequence: | MALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMF
DMECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISI
AEDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYS
MDVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICV
FPREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSI
IFIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVV
NETLRLFPIAMRLERVCKKDVEINGMFIPKGVVVMIPSYALHRDPKYWTEPEKFLPERFS
KKNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLG
GLLQPEKPVVLKVESRDGTVSGA
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BDBM50078374 |
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n/a |
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Name | BDBM50078374 |
Synonyms: | CHEMBL3414926 |
Type | Small organic molecule |
Emp. Form. | C24H22FN5O3 |
Mol. Mass. | 447.4616 |
SMILES | COCCOc1cnc2ccc(cc2c1)[C@H](C)c1nnc2c(F)cc(cn12)-c1cc(C)no1 |r| |
Structure |
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