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TargetSerine/threonine-protein kinase B-raf
LigandBDBM202784
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1663100 (CHEMBL4012781)
IC50 0.400000±n/a nM
Citation Nishiguchi, GARico, ATanner, HAversa, RJTaft, BRSubramanian, SSetti, LBurger, MTWan, LTamez, VSmith, ALou, YBarsanti, PAAppleton, BAMamo, MTandeske, LDix, ITellew, JEHuang, SMathews Griner, LACooke, VGVan Abbema, AMerritt, HMa, SGampa, KFeng, FYuan, JWang, YHaling, JRVaziri, SHekmat-Nejad, MJansen, JMPolyakov, VZang, RSethuraman, VAmiri, PSingh, MLees, EShao, WStuart, DDDillon, MPRamurthy, S Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem60:4869-4881 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase B-raf
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:
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATV
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM202784
n/a
NameBDBM202784
Synonyms:US10245267, Example 131 | US10709712, Example 131 | US9242969, 131 | US9694016, 131
TypeSmall organic molecule
Emp. Form.C28H29F3N4O4
Mol. Mass.542.5495
SMILESCc1ncc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1cnc(OC2CCOCC2)c(c1)N1CCOCC1
Structure
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