Reaction Details |
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Target | Serine/threonine-protein kinase B-raf [V600E] |
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Ligand | BDBM202665 |
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Substrate/Competitor | MEK1 (K97R) |
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Meas. Tech. | Raf Activity Assay |
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pH | 7.5±n/a |
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Temperature | 298.15±n/a K |
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IC50 | 0.30±n/a nM |
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Comments | extracted |
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Citation | Aversa, RJ; Barsanti, PA; Burger, M; Dillon, MP; Dipesa, A; Hu, C; Lou, Y; Nishiguchi, G; Pan, Y; Polyakov, V; Ramurthy, S; Rico, A; Setti, L; Smith, A; Subramanian, S; Taft, B; Tanner, H; Wan, L; Yusuff, N Biaryl amide compounds as kinase inhibitors US Patent US9694016 Publication Date 7/4/2017 |
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More Info.: | Get all data from this article, 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] |
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) |
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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BDBM202665 |
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MEK1 (K97R) |
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Name: | Dual specificity mitogen-activated protein kinase kinase 1 [K97R] |
Synonyms: | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1)(K97R) | MAP2K1 | MEK1 | MEK1 (K97R) | MP2K1_HUMAN | PRKMK1 |
Type: | n/a |
Mol. Mass.: | 43467.04 |
Organism: | Homo sapiens (Human) |
Description: | Biotinylated full length MEK1 with an inactivating K97R ATP binding site mutation. |
Residue: | 393 |
Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARRLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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