| Reaction Details |
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 | Report a problem with these data |
| Target | Glutaminase kidney isoform, mitochondrial |
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| Ligand | BDBM50514985 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1859477 (CHEMBL4360333) |
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| IC50 | 10.0±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 kidney isoform, mitochondrial |
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| Name: | Glutaminase kidney isoform, mitochondrial |
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| Synonyms: | GLS | GLS1 | GLSK_HUMAN | Glutaminase 1 | K-glutaminase | KIAA0838 | L-glutamine amidohydrolase |
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| Type: | Protein |
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| Mol. Mass.: | 73471.89 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O94925 |
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| Residue: | 669 |
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| Sequence: | MMRLRGSGMLRDLLLRSPAGVSATLRRAQPLVTLCRRPRGGGRPAAGPAAAARLHPWWGG
GGWPAEPLARGLSSSPSEILQELGKGSTHPQPGVSPPAAPAAPGPKDGPGETDAFGNSEG
KELVASGENKIKQGLLPSLEDLLFYTIAEGQEKIPVHKFITALKSTGLRTSDPRLKECMD
MLRLTLQTTSDGVMLDKDLFKKCVQSNIVLLTQAFRRKFVIPDFMSFTSHIDELYESAKK
QSGGKVADYIPQLAKFSPDLWGVSVCTVDGQRHSTGDTKVPFCLQSCVKPLKYAIAVNDL
GTEYVHRYVGKEPSGLRFNKLFLNEDDKPHNPMVNAGAIVVTSLIKQGVNNAEKFDYVMQ
FLNKMAGNEYVGFSNATFQSERESGDRNFAIGYYLKEKKCFPEGTDMVGILDFYFQLCSI
EVTCESASVMAATLANGGFCPITGERVLSPEAVRNTLSLMHSCGMYDFSGQFAFHVGLPA
KSGVAGGILLVVPNVMGMMCWSPPLDKMGNSVKGIHFCHDLVSLCNFHNYDNLRHFAKKL
DPRREGGDQRVKSVINLLFAAYTGDVSALRRFALSAMDMEQRDYDSRTALHVAAAEGHVE
VVKFLLEACKVNPFPKDRWNNTPMDEALHFGHHDVFKILQEYQVQYTPQGDSDNGKENQT
VHKNLDGLL
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| BDBM50514985 |
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| n/a |
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| Name | BDBM50514985 |
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| Synonyms: | CHEMBL4573635 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H21N7OS |
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| Mol. Mass. | 395.481 |
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| SMILES | C[C@H](C(=O)Nc1nnc(N[C@@H]2CCN(C2)c2cccnn2)s1)c1ccccc1 |r| |
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| Structure | 
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