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TargetB-RAF V600E
LigandBDBM35326
Substrate/Competitorbiotin-MEK
Meas. Tech.In Vitro BRAF Kinase Assay
pH7±n/a
Temperature296.15±n/a K
IC50 21±n/a nM
EC50 27±n/a nM
Citation Smith, ALDeMorin, FFParas, NAHuang, QPetkus, JKDoherty, EMNixey, TKim, JLWhittington, DAEpstein, LFLee, MRRose, MJBabij, CFernando, MHess, KLe, QBeltran, PCarnahan, J Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. J Med Chem52:6189-92 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
B-RAF V600E
Name:B-RAF V600E
Synonyms:B-Raf (V600E) | B-Raf Protein Kinase Mutant (V600E) | B-Raf proto-oncogene serine/threonine-protein kinase | BRAF (V600E) | BRAF mutant V600E | P15056 | Protein mono-ADP-ribosyltransferase (PARP3) | RAF serine/threonine protein kinase (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:
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATE
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
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BDBM35326
NameBDBM35326
Synonyms:aminoquinazoline, 20
TypeSmall organic molecule
Emp. Form.C29H26N6O
Mol. Mass.474.5563
SMILESCNc1ncc2cc(ccc2n1)-c1c(C)ccc2c(Nc3ccc4c(NC(=O)C4(C)C)c3)nccc12
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
biotin-MEK
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:
n/a