| Reaction Details |
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 | Report a problem with these data |
| Target | Serine/threonine-protein kinase B-raf [V600E] |
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| Ligand | BDBM16673 |
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| Substrate/Competitor | Dual specificity mitogen-activated protein kinase kinase 1 |
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| Meas. Tech. | B-RAF (V600E) Kinase Inhibition Assay |
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| pH | 7.2±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 43±n/a nM |
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| Citation |  Niculescu-Duvaz, D; Gaulon, C; Dijkstra, HP; Niculescu-Duvaz, I; Zambon, A; Ménard, D; Suijkerbuijk, BM; Nourry, A; Davies, L; Manne, H; Friedlos, F; Ogilvie, L; Hedley, D; Whittaker, S; Kirk, R; Gill, A; Taylor, RD; Raynaud, FI; Moreno-Farre, J; Marais, R; Springer, CJ Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF). J Med Chem52:2255-64 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Serine/threonine-protein kinase B-raf [V600E] |
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| Name: | Serine/threonine-protein kinase B-raf [V600E] |
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| Synonyms: | B-RAF V600E | B-Raf (V600E) | B-Raf Protein Kinase Mutant (V600E) | B-Raf proto-oncogene serine/threonine-protein kinase | BRAF | BRAF (V600E) | BRAF mutant V600E | BRAF1 | BRAF_HUMAN | P15056 | Protein mono-ADP-ribosyltransferase (PARP3) | RAF serine/threonine protein kinase (V600E) | RAFB1 | Serine/threonine-protein kinase B-raf (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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| BDBM16673 |
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| Dual specificity mitogen-activated protein kinase kinase 1 |
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| Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
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| Synonyms: | GST fusion of MAP kinase kinase 1 | GST-MEK1 | MAP2K1 | MEK1 | MP2K1_RABIT | PRKMK1 | glutathione S-transferase-MAP kinase kinase 1 |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 43453 |
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| Organism: | Oryctolagus cuniculus (rabbit) |
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| Description: | Rabbit MEK1 was purchased from Millipore. |
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| Residue: | 393 |
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| Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSAVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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