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Target
Serine/threonine-protein kinase B-raf
Ligand
BDBM50428286
Substrate
n/a
Meas. Tech.
ChEMBL_1495598 (CHEMBL3578336)
IC50
9.7±n/a nM
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 Chem 58:4165-79 (2015) [PubMed]  Article 
Target
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:
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQRDRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSPGPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDVAVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATVKSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNINNRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARSLPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
  
Inhibitor
Name:
BDBM50428286
Synonyms:
DABRAFENIB | GSK2118436A
Type:
Small organic molecule
Emp. Form.:
C23H20F3N5O2S2
Mol. Mass.:
519.562
SMILES:
CC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F
Structure:
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