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TargetSerine/threonine-protein kinase B-raf
LigandBDBM50396483
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1495597 (CHEMBL3578335)
IC50 6.1±n/a nM
Citation Henry, JRKaufman, MDPeng, SBAhn, YMCaldwell, TMVogeti, LTelikepalli, HLu, WPHood, MMRutkoski, TJSmith, BDVogeti, SMiller, DWise, SCChun, LZhang, XZhang, YKays, LHipskind, PAWrobleski, ADLobb, KLClay, JMCohen, JDWalgren, JLMcCann, DPatel, PClawson, DKGuo, SManglicmot, DGroshong, CLogan, CStarling, JJFlynn, 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
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase B-raf
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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  Blast E-value cutoff:
BDBM50396483
n/a
NameBDBM50396483
Synonyms:PLX-4032 | RG 7204 | Ro 5185426 | US10570155, Vemurafenib | US11332479, Compound Vemurafenib | US11492357, Control | US9388165, Reference, Vemurafenib (PLX-4032) | USRE47451, PLX-4032, Roche | VEMURAFENIB
TypeSmall organic molecule
Emp. Form.C23H18ClF2N3O3S
Mol. Mass.489.922
SMILESCCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(cc23)-c2ccc(Cl)cc2)c1F
Structure
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