| Reaction Details |
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 | Report a problem with these data |
| Target | B-RAF V600E |
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| Ligand | BDBM35326 |
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| Substrate/Competitor | biotin-MEK |
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| Meas. Tech. | In Vitro BRAF Kinase Assay |
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| pH | 7±n/a |
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| Temperature | 296.15±n/a K |
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| IC50 | 21±n/a nM |
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| EC50 | 27±n/a nM |
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| Citation |  Smith, AL; DeMorin, FF; Paras, NA; Huang, Q; Petkus, JK; Doherty, EM; Nixey, T; Kim, JL; Whittington, DA; Epstein, LF; Lee, MR; Rose, MJ; Babij, C; Fernando, M; Hess, K; Le, Q; Beltran, P; Carnahan, 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 |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| B-RAF V600E |
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| Name: | B-RAF V600E |
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| 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) |
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| Type: | n/a |
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| Mol. Mass.: | 84474.98 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P15056 V600E |
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| Residue: | 766 |
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| Sequence: | MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATE
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
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| BDBM35326 |
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| Name | BDBM35326 |
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| Synonyms: | aminoquinazoline, 20 |
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| Type | Small organic molecule |
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| Emp. Form. | C29H26N6O |
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| Mol. Mass. | 474.5563 |
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| SMILES | CNc1ncc2cc(ccc2n1)-c1c(C)ccc2c(Nc3ccc4c(NC(=O)C4(C)C)c3)nccc12 |
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| Structure | 
|
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| biotin-MEK |
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| Name: | biotin-MEK |
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| Synonyms: | n/a |
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| Type: | biotinylated substrate |
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| Mol. Mass.: | 358.43 |
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| Organism: | n/a |
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| Description: | Perkin-Elmer s AlphaScreen assay kit. |
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| Residue: | 3 |
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| Sequence: | |
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