| 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 | BDBM50428286 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1495745 (CHEMBL3578908) |
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| IC50 | 150±n/a nM |
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| Citation |  Henry, JR; Kaufman, MD; Peng, SB; Ahn, YM; Caldwell, TM; Vogeti, L; Telikepalli, H; Lu, WP; Hood, MM; Rutkoski, TJ; Smith, BD; Vogeti, S; Miller, D; Wise, SC; Chun, L; Zhang, X; Zhang, Y; Kays, L; Hipskind, PA; Wrobleski, AD; Lobb, KL; Clay, JM; Cohen, JD; Walgren, JL; McCann, D; Patel, P; Clawson, DK; Guo, S; Manglicmot, D; Groshong, C; Logan, C; Starling, JJ; Flynn, DL Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. J Med Chem58:4165-79 (2015) [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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| BDBM50428286 |
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| n/a |
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| Name | BDBM50428286 |
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| Synonyms: | DABRAFENIB | GSK2118436A |
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| Type | Small organic molecule |
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| Emp. Form. | C23H20F3N5O2S2 |
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| Mol. Mass. | 519.562 |
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| SMILES | CC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F |
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| Structure | 
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