Reaction Details |
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Target | Serine/threonine-protein kinase B-raf |
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Ligand | BDBM50482019 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_624870 (CHEMBL1104358) |
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IC50 | 1970±n/a nM |
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Citation | Suijkerbuijk, BM; Niculescu-Duvaz, I; Gaulon, C; Dijkstra, HP; Niculescu-Duvaz, D; Ménard, D; Zambon, A; Nourry, A; Davies, L; Manne, HA; Friedlos, F; Ogilvie, LM; Hedley, D; Lopes, F; Preece, NP; Moreno-Farre, J; Raynaud, FI; Kirk, R; Whittaker, S; Marais, R; Springer, CJ Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group. J Med Chem53:2741-56 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase B-raf |
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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
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BDBM50482019 |
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n/a |
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Name | BDBM50482019 |
Synonyms: | CHEMBL1092523 |
Type | Small organic molecule |
Emp. Form. | C25H23N7O3 |
Mol. Mass. | 469.4952 |
SMILES | CC(C)c1cc(NC(=O)Nc2ccc(Oc3ccnc4[nH]c(=O)[nH]c34)cc2)n(n1)-c1ccccc1 |
Structure |
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