Reaction Details |
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Target | Serine/threonine-protein kinase B-raf |
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Ligand | BDBM202784 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1663100 (CHEMBL4012781) |
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IC50 | 0.400000±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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Serine/threonine-protein kinase B-raf |
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Name: | Serine/threonine-protein kinase B-raf |
Synonyms: | B-RAF | B-Raf Protein Kinase | B-Raf proto-oncogene serine/threonine-protein kinase | BRAF | BRAF1 | BRAF_HUMAN | RAFB1 | p94 | v-Raf murine sarcoma viral oncogene homolog B1 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 84446.00 |
Organism: | Homo sapiens (Human) |
Description: | P15056 |
Residue: | 766 |
Sequence: | MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATV
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
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BDBM202784 |
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n/a |
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Name | BDBM202784 |
Synonyms: | US10245267, Example 131 | US10709712, Example 131 | US9242969, 131 | US9694016, 131 |
Type | Small organic molecule |
Emp. Form. | C28H29F3N4O4 |
Mol. Mass. | 542.5495 |
SMILES | Cc1ncc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1cnc(OC2CCOCC2)c(c1)N1CCOCC1 |
Structure |
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