Reaction Details |
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Target | Isocitrate dehydrogenase [NADP] cytoplasmic [R132C] |
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Ligand | BDBM375169 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Cellular 2-HG Assay Using HCT116 Mutant IDH1 Cells |
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IC50 | 55±n/a nM |
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Citation | Lin, J; Ericsson, A; Campbell, A; Gustafson, G; Wang, Z; Diebold, RB; Ashwell, S; Lancia, Jr., DR; Caravella, JA; Lu, W Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors US Patent US10253015 Publication Date 4/9/2019 |
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More Info.: | Get all data from this article, Assay Method |
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Isocitrate dehydrogenase [NADP] cytoplasmic [R132C] |
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Name: | Isocitrate dehydrogenase [NADP] cytoplasmic [R132C] |
Synonyms: | IDH1 | IDH1 R132C | IDH1(R132C) | IDHC_HUMAN | Isocitrate dehydrogenase (IDH1)(R132C) | Isocitrate dehydrogenase 1 mutant (R132C) | Isocitrate dehydrogenase [NADP] cytoplasmic (IDH1) (R132C) | PICD |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 46607.23 |
Organism: | Homo sapiens (Human) |
Description: | O75874[R132C] |
Residue: | 414 |
Sequence: | MSKKISGGSVVEMQGDEMTRIIWELIKEKLIFPYVELDLHSYDLGIENRDATNDQVTKDA
AEAIKKHNVGVKCATITPDEKRVEEFKLKQMWKSPNGTIRNILGGTVFREAIICKNIPRL
VSGWVKPIIIGCHAYGDQYRATDFVVPGPGKVEITYTPSDGTQKVTYLVHNFEEGGGVAM
GMYNQDKSIEDFAHSSFQMALSKGWPLYLSTKNTILKKYDGRFKDIFQEIYDKQYKSQFE
AQKIWYEHRLIDDMVAQAMKSEGGFIWACKNYDGDVQSDSVAQGYGSLGMMTSVLVCPDG
KTVEAEAAHGTVTRHYRMYQKGQETSTNPIASIFAWTRGLAHRAKLDNNKELAFFANALE
EVSIETIEAGFMTKDLAACIKGLPNVQRSDYLNTFEFMDKLGENLKIKLAQAKL
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BDBM375169 |
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n/a |
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Name | BDBM375169 |
Synonyms: | 6-({1-[6-chloro-2-oxo-7- | US10253015, Compound I-29 |
Type | Small organic molecule |
Emp. Form. | C24H20ClN5O2 |
Mol. Mass. | 445.901 |
SMILES | CC(Nc1ccc(C#N)c(C)n1)c1cc2cc(Cl)c(OCc3ccccn3)cc2[nH]c1=O |
Structure |
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