Reaction Details |
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Target | Isocitrate dehydrogenase [NADP] cytoplasmic [R132G] |
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Ligand | BDBM195601 |
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Substrate/Competitor | n/a |
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Meas. Tech. | RapidFire-MS/MS and NADPH Assays |
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Temperature | 298.15±n/a K |
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IC50 | 2.9±0.0 nM |
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Comments | extracted |
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Citation | Okoye-Okafor, UC; Bartholdy, B; Cartier, J; Gao, EN; Pietrak, B; Rendina, AR; Rominger, C; Quinn, C; Smallwood, A; Wiggall, KJ; Reif, AJ; Schmidt, SJ; Qi, H; Zhao, H; Joberty, G; Faelth-Savitski, M; Bantscheff, M; Drewes, G; Duraiswami, C; Brady, P; Groy, A; Narayanagari, SR; Antony-Debre, I; Mitchell, K; Wang, HR; Kao, YR; Christopeit, M; Carvajal, L; Barreyro, L; Paietta, E; Makishima, H; Will, B; Concha, N; Adams, ND; Schwartz, B; McCabe, MT; Maciejewski, J; Verma, A; Steidl, U New IDH1 mutant inhibitors for treatment of acute myeloid leukemia Nat Chem Biol11:878-86 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Isocitrate dehydrogenase [NADP] cytoplasmic [R132G] |
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Name: | Isocitrate dehydrogenase [NADP] cytoplasmic [R132G] |
Synonyms: | IDH1 | IDHC_HUMAN | Isocitrate dehydrogenase 1 mutant (R132G) | PICD |
Type: | Protein |
Mol. Mass.: | 46561.14 |
Organism: | Homo sapiens (Human) |
Description: | R132G mutant |
Residue: | 414 |
Sequence: | MSKKISGGSVVEMQGDEMTRIIWELIKEKLIFPYVELDLHSYDLGIENRDATNDQVTKDA
AEAIKKHNVGVKCATITPDEKRVEEFKLKQMWKSPNGTIRNILGGTVFREAIICKNIPRL
VSGWVKPIIIGGHAYGDQYRATDFVVPGPGKVEITYTPSDGTQKVTYLVHNFEEGGGVAM
GMYNQDKSIEDFAHSSFQMALSKGWPLYLSTKNTILKKYDGRFKDIFQEIYDKQYKSQFE
AQKIWYEHRLIDDMVAQAMKSEGGFIWACKNYDGDVQSDSVAQGYGSLGMMTSVLVCPDG
KTVEAEAAHGTVTRHYRMYQKGQETSTNPIASIFAWTRGLAHRAKLDNNKELAFFANALE
EVSIETIEAGFMTKDLAACIKGLPNVQRSDYLNTFEFMDKLGENLKIKLAQAKL
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BDBM195601 |
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n/a |
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Name | BDBM195601 |
Synonyms: | GSK321 | US11311527, Cpd ID GSK321 | US11376246, Cpd ID GSK321 | US11576906, Compound GSK321 |
Type | Small organic molecule |
Emp. Form. | C28H28FN5O3 |
Mol. Mass. | 501.552 |
SMILES | C[C@H](O)c1cccc(NC(=O)c2nn(Cc3ccc(F)cc3)c3[C@H](C)CN(Cc23)C(=O)c2ccc[nH]2)c1 |r| |
Structure |
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