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Target
Serine/threonine-protein kinase B-raf
Ligand
BDBM25653
Substrate
GST-MEK
Meas. Tech.
B-Raf Activity Assay
IC50
1.5±n/a nM
Citation
 Hansen, JD; Grina, J; Newhouse, B; Welch, M; Topalov, G; Littman, N; Callejo, M; Gloor, S; Martinson, M; Laird, E; Brandhuber, BJ; Vigers, G; Morales, T; Woessner, R; Randolph, N; Lyssikatos, J; Olivero, A Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett 18:4692-5 (2008) [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:
BDBM25653
Synonyms:
4-(4-{2H,4H-indeno[1,2-c]pyrazol-6-yl}-1-methyl-1H-pyrazol-3-yl)pyridine | pyrazole-based inhibitor, 35
Type:
Small organic molecule
Emp. Form.:
C19H15N5
Mol. Mass.:
313.3559
SMILES:
Cn1cc(c(n1)-c1ccncc1)-c1ccc-2c(Cc3c[nH]nc-23)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
GST-MEK
Synonyms:
GST-kdMEK
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
n/a
Description:
This protein is purified from bacterial cells expression mutant inactive MEK as a fusion protein with glutathione-S-transferase (GST-kdMEK).
Residue:
3
Sequence:
NA