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Target
Serine/threonine-protein kinase B-raf [V600E]
Ligand
BDBM25617
Substrate
biotin-MEK
Meas. Tech.
In Vitro BRAF Kinase Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
13±n/a nM
Citation
 Tsai, J; Lee, JT; Wang, W; Zhang, J; Cho, H; Mamo, S; Bremer, R; Gillette, S; Kong, J; Haass, NK; Sproesser, K; Li, L; Smalley, KS; Fong, D; Zhu, YL; Marimuthu, A; Nguyen, H; Lam, B; Liu, J; Cheung, I; Rice, J; Suzuki, Y; Luu, C; Settachatgul, C; Shellooe, R; Cantwell, J; Kim, SH; Schlessinger, J; Zhang, KY; West, BL; Powell, B; Habets, G; Zhang, C; Ibrahim, PN; Hirth, P; Artis, DR; Herlyn, M; Bollag, G Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A 105:3041-6 (2008) [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:
BDBM25617
Synonyms:
N-[3-({5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl}carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide | PLX4720
Type:
Small organic molecule
Emp. Form.:
C17H14ClF2N3O3S
Mol. Mass.:
413.826
SMILES:
CCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(Cl)cc23)c1F
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