Reaction Details |
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Target | Serine/threonine-protein kinase B-raf |
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Ligand | BDBM50482448 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_646978 (CHEMBL1217119) |
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IC50 | 21±n/a nM |
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Citation | Zambon, A; Ménard, D; Suijkerbuijk, BM; Niculescu-Duvaz, I; Whittaker, S; Niculescu-Duvaz, D; Nourry, A; Davies, L; Manne, HA; Lopes, F; Preece, N; Hedley, D; Ogilvie, LM; Kirk, R; Marais, R; Springer, CJ Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors. J Med Chem53:5639-55 (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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BDBM50482448 |
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n/a |
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Name | BDBM50482448 |
Synonyms: | CHEMBL1213822 |
Type | Small organic molecule |
Emp. Form. | C21H13ClF3N5O4 |
Mol. Mass. | 491.807 |
SMILES | FC(F)(F)c1cc(NC(=O)Nc2ccc(Oc3ccnc4[nH]c(=O)c(=O)[nH]c34)cc2)ccc1Cl |
Structure |
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