Reaction Details |
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Target | Glutaminase liver isoform, mitochondrial |
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Ligand | BDBM50514983 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1859478 (CHEMBL4360334) |
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IC50 | >40000±n/a nM |
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Citation | Finlay, MRV; Anderton, M; Bailey, A; Boyd, S; Brookfield, J; Cairnduff, C; Charles, M; Cheasty, A; Critchlow, SE; Culshaw, J; Ekwuru, T; Hollingsworth, I; Jones, N; Leroux, F; Littleson, M; McCarron, H; McKelvie, J; Mooney, L; Nissink, JWM; Perkins, D; Powell, S; Quesada, MJ; Raubo, P; Sabin, V; Smith, J; Smith, PD; Stark, A; Ting, A; Wang, P; Wilson, Z; Winter-Holt, JJ; Wood, JM; Wrigley, GL; Yu, G; Zhang, P Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models. J Med Chem62:6540-6560 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glutaminase liver isoform, mitochondrial |
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Name: | Glutaminase liver isoform, mitochondrial |
Synonyms: | 3.5.1.2 | GA | GLS | GLS2 | GLSL_HUMAN | Glutaminase liver isoform, mitochondrial | L-glutaminase | L-glutamine amidohydrolase |
Type: | PROTEIN |
Mol. Mass.: | 66331.64 |
Organism: | Homo sapiens |
Description: | ChEMBL_117753 |
Residue: | 602 |
Sequence: | MRSMKALQKALSRAGSHCGRGGWGHPSRSPLLGGGVRHHLSEAAAQGRETPHSHQPQHQD
HDSSESGMLSRLGDLLFYTIAEGQERIPIHKFTTALKATGLQTSDPRLRDCMSEMHRVVQ
ESSSGGLLDRDLFRKCVSSNIVLLTQAFRKKFVIPDFEEFTGHVDRIFEDVKELTGGKVA
AYIPQLAKSNPDLWGVSLCTVDGQRHSVGHTKIPFCLQSCVKPLTYAISISTLGTDYVHK
FVGKEPSGLRYNKLSLNEEGIPHNPMVNAGAIVVSSLIKMDCNKAEKFDFVLQYLNKMAG
NEYMGFSNATFQSEKETGDRNYAIGYYLKEKKCFPKGVDMMAALDLYFQLCSVEVTCESG
SVMAATLANGGICPITGESVLSAEAVRNTLSLMHSCGMYDFSGQFAFHVGLPAKSAVSGA
ILLVVPNVMGMMCLSPPLDKLGNSHRGTSFCQKLVSLFNFHNYDNLRHCARKLDPRREGA
EIRNKTVVNLLFAAYSGDVSALRRFALSAMDMEQKDYDSRTALHVAAAEGHIEVVKFLIE
ACKVNPFAKDRWGNIPLDDAVQFNHLEVVKLLQDYQDSYTLSETQAEAAAEALSKENLES
MV
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BDBM50514983 |
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n/a |
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Name | BDBM50514983 |
Synonyms: | CHEMBL4447951 |
Type | Small organic molecule |
Emp. Form. | C17H18N8OS |
Mol. Mass. | 382.443 |
SMILES | O=C(Cc1ccccc1)Nc1nnc(N[C@@H]2CCN(C2)c2nccnn2)s1 |r| |
Structure |
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