Target
Serine/threonine-protein kinase B-raf [V600E]
Ligand
BDBM88086
Substrate
n/a
Meas. Tech.
In Vitro Activity Assay
IC50
2.00±n/a nM
Citation
 Aversa, RJBarsanti, PABurger, MTDillon, MPDipesa, AHu, CLou, YNishiguchi, GAPan, YPolyakov, VRRamurthy, SRico, ACSetti, LQSmith, ASubramanian, STaft, BRTanner, HRWan, LYusuff, N Biaryl amide compounds as kinase inhibitors US Patent  US10709712 Publication Date 7/14/2020 
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:
BDBM88086
Synonyms:
US10245267, Example 1119 | US10709712, Example 1119 | US9694016, 1119
Type:
Small organic molecule
Emp. Form.:
C28H34N6O3
Mol. Mass.:
502.608
SMILES:
CC(C)c1cc(ccn1)C(=O)Nc1cnc(C)c(c1)-c1cc(nc(c1)N1CCOCC1)N1CCOCC1
Structure:
Search PDB for entries with ligand similarity: