Target
Serine/threonine-protein kinase A-Raf
Ligand
BDBM50396483
Substrate
n/a
Meas. Tech.
ChEMBL_1699091 (CHEMBL4050073)
IC50
2.1±n/a nM
Citation
 Wang, LZhang, QZhu, GZhang, ZZhi, YZhang, LMao, TZhou, XChen, YLu, TTang, W Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance. Eur J Med Chem 130:86-106 (2017) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase A-Raf
Synonyms:
ARAF | ARAF1 | ARAF_HUMAN | PKS | PKS2 | Proto-oncogene A-Raf | Proto-oncogene A-Raf-1 | Proto-oncogene Pks | RAF serine/threonine protein kinase
Type:
Enzyme
Mol. Mass.:
67610.81
Organism:
Homo sapiens (Human)
Description:
P10398
Residue:
606
Sequence:
MEPPRGPPANGAEPSRAVGTVKVYLPNKQRTVVTVRDGMSVYDSLDKALKVRGLNQDCCVVYRLIKGRKTVTAWDTAIAPLDGEELIVEVLEDVPLTMHNFVRKTFFSLAFCDFCLKFLFHGFRCQTCGYKFHQHCSSKVPTVCVDMSTNRQQFYHSVQDLSGGSRQHEAPSNRPLNELLTPQGPSPRTQHCDPEHFPFPAPANAPLQRIRSTSTPNVHMVSTTAPMDSNLIQLTGQSFSTDAAGSRGGSDGTPRGSPSPASVSSGRKSPHSKSPAEQRERKSLADDKKKVKNLGYRDSGYYWEVPPSEVQLLKRIGTGSFGTVFRGRWHGDVAVKVLKVSQPTAEQAQAFKNEMQVLRKTRHVNILLFMGFMTRPGFAIITQWCEGSSLYHHLHVADTRFDMVQLIDVARQTAQGMDYLHAKNIIHRDLKSNNIFLHEGLTVKIGDFGLATVKTRWSGAQPLEQPSGSVLWMAAEVIRMQDPNPYSFQSDVYAYGVVLYELMTGSLPYSHIGCRDQIIFMVGRGYLSPDLSKISSNCPKAMRRLLSDCLKFQREERPLFPQILATIELLQRSLPKIERSASEPSLHRTQADELPACLLSAARLVP
  
Inhibitor
Name:
BDBM50396483
Synonyms:
PLX-4032 | RG 7204 | Ro 5185426 | US10570155, Vemurafenib | US11332479, Compound Vemurafenib | US11492357, Control | US9388165, Reference, Vemurafenib (PLX-4032) | USRE47451, PLX-4032, Roche | VEMURAFENIB
Type:
Small organic molecule
Emp. Form.:
C23H18ClF2N3O3S
Mol. Mass.:
489.922
SMILES:
CCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(cc23)-c2ccc(Cl)cc2)c1F
Structure:
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