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Target
Serine/threonine-protein kinase B-raf [V600E]
Ligand
BDBM35318
Substrate
biotin-MEK
Meas. Tech.
In Vitro BRAF Kinase Assay
pH
7±n/a
Temperature
296.15±n/a K
IC50
17±n/a nM
EC50
53±n/a nM
Citation
 Smith, AL; DeMorin, FF; Paras, NA; Huang, Q; Petkus, JK; Doherty, EM; Nixey, T; Kim, JL; Whittington, DA; Epstein, LF; Lee, MR; Rose, MJ; Babij, C; Fernando, M; Hess, K; Le, Q; Beltran, P; Carnahan, J Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. J Med Chem 52:6189-92 (2009) [PubMed]  Article 
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:
BDBM35318
Synonyms:
aminoisoquinoline, 12a
Type:
Small organic molecule
Emp. Form.:
C26H19F3N6
Mol. Mass.:
472.4645
SMILES:
Cc1ccc2c(Nc3cccc(c3)C(F)(F)F)nccc2c1Nc1ncccc1-c1ccncn1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotin-MEK
Synonyms:
n/a
Type:
biotinylated substrate
Mol. Mass.:
358.43
Organism:
n/a
Description:
Perkin-Elmer s AlphaScreen assay kit.
Residue:
3
Sequence:
NA