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Target
Serine/threonine-protein kinase B-raf
Ligand
BDBM25622
Substrate
GST-MEK
Meas. Tech.
B-Raf Activity Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
3.46±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:
BDBM25622
Synonyms:
(1Z)-5-[1-cyclopentyl-3-(pyridin-4-yl)-1H-pyrazol-4-yl]-2,3-dihydro-1H-indene-1-hydroxylamine | pyrazole-based inhibitor, 4
Type:
Small organic molecule
Emp. Form.:
C22H22N4O
Mol. Mass.:
358.4363
SMILES:
O=NC1CCc2cc(ccc12)-c1cn(nc1-c1ccncc1)C1CCCC1
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