Target
Serine/threonine-protein kinase B-raf [V600E]
Ligand
BDBM333649
Substrate
n/a
Meas. Tech.
Competition Binding Assay
Kd
>1000±n/a nM
Citation
 Abraham, SBhagwat, SSCampbell, BTChao, QFaraoni, RHolladay, MWLai, AGRowbottom, MWSetti, ESprankle, KG RAF kinase modulator compounds and methods of use thereof US Patent  US9730937 Publication Date 8/15/2017 
Target
Name:
Serine/threonine-protein kinase B-raf [V600E]
Synonyms:
B-RAF V600E | B-Raf (V600E) | B-Raf Protein Kinase Mutant (V600E) | B-Raf proto-oncogene serine/threonine-protein kinase | BRAF | BRAF (V600E) | BRAF mutant V600E | BRAF1 | BRAF_HUMAN | P15056 | Protein mono-ADP-ribosyltransferase (PARP3) | RAF serine/threonine protein kinase (V600E) | RAFB1 | Serine/threonine-protein kinase B-raf (V600E) | Serine/threonine-protein kinase B-raf (V600E) | Serine/threonine-protein kinase B-raf [V600E] | V-RAF murine sarcoma viral oncogene homologue B1 mutant (BRAF V600E)
Type:
n/a
Mol. Mass.:
84474.98
Organism:
Homo sapiens (Human)
Description:
P15056 V600E
Residue:
766
Sequence:
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQRDRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSPGPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDVAVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATEKSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNINNRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARSLPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
  
Inhibitor
Name:
BDBM333649
Synonyms:
1-[3-(6,7- dimethoxy- quinazolin- 4- ylthio)phenyl]- 3-[1- (4- fluorophenyl)-3- (trifluoromethyl)- 1H- pyrazol-5-yl] urea | US9730937, Example 198 | US9730937, Example 199
Type:
Small organic molecule
Emp. Form.:
C27H20F4N6O3S
Mol. Mass.:
584.545
SMILES:
COc1cc2ncnc(Sc3cccc(NC(=O)Nc4cc(nn4-c4ccc(F)cc4)C(F)(F)F)c3)c2cc1OC
Structure:
Search PDB for entries with ligand similarity: