| Reaction Details |
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 | Report a problem with these data |
| Target | RAF proto-oncogene serine/threonine-protein kinase |
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| Ligand | BDBM202770 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1663046 (CHEMBL4012727) |
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| EC50 | 76±n/a nM |
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| Citation |  Nishiguchi, GA; Rico, A; Tanner, H; Aversa, RJ; Taft, BR; Subramanian, S; Setti, L; Burger, MT; Wan, L; Tamez, V; Smith, A; Lou, Y; Barsanti, PA; Appleton, BA; Mamo, M; Tandeske, L; Dix, I; Tellew, JE; Huang, S; Mathews Griner, LA; Cooke, VG; Van Abbema, A; Merritt, H; Ma, S; Gampa, K; Feng, F; Yuan, J; Wang, Y; Haling, JR; Vaziri, S; Hekmat-Nejad, M; Jansen, JM; Polyakov, V; Zang, R; Sethuraman, V; Amiri, P; Singh, M; Lees, E; Shao, W; Stuart, DD; Dillon, MP; Ramurthy, S Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem60:4869-4881 (2017) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| RAF proto-oncogene serine/threonine-protein kinase |
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| Name: | RAF proto-oncogene serine/threonine-protein kinase |
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| Synonyms: | C-Raf Protein Kinase | Proto-oncogene c-RAF (RAF1) | RAF | RAF proto-oncogene
serine/threonine-protein kinase (C-Raf) | RAF1 | RAF1_HUMAN | Raf-1 | Serine/threonine-protein kinase
RAF | Serine/threonine-protein kinase C-Raf | cRaf |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 73082.52 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P04049 |
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| Residue: | 648 |
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| Sequence: | MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRV
FLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAAS
LIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKV
PTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTF
NTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNL
SPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSYYWEIEASEVMLSTRIGSGSF
GTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIV
TQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGL
TVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYE
LMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFP
QILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
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| BDBM202770 |
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| n/a |
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| Name | BDBM202770 |
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| Synonyms: | US10245267, Example 117 | US10709712, Example 117 | US9242969, 117 | US9694016, 117 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H24F3N3O3 |
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| Mol. Mass. | 471.4716 |
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| SMILES | Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1cc(N2CCOCC2)c(=O)n(C)c1 |
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| Structure | 
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