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Target
Serine/threonine-protein kinase B-raf [V600E]
Ligand
BDBM77857
Substrate
n/a
Meas. Tech.
In Vitro Raf Activity
IC50
3.20±n/a nM
Citation
 Aversa, RJ; Barsanti, PA; Burger, MT; Dillon, MP; Dipesa, A; Hu, C; Lou, Y; Nishiguchi, GA; Pan, Y; Polyakov, VR; Ramurthy, S; Rico, AC; Setti, LQ; Smith, A; Subramanian, S; Taft, BR; Tanner, HR; Wan, L; Yusuff, N Biaryl amide compounds as kinase inhibitors US Patent  US10245267 Publication Date 4/2/2019 
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:
BDBM77857
Synonyms:
US10245267, Example 301 | US10709712, Example 301 | US9694016, 301
Type:
Small organic molecule
Emp. Form.:
C24H24F3N5O4
Mol. Mass.:
503.4737
SMILES:
Cc1ncc(NC(=O)c2cc(ccn2)C(F)(F)F)cc1-c1cnc(OCCO)c(c1)N1CCOCC1
Structure:
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