Reaction Details |
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Target | Glutaminase kidney isoform, mitochondrial |
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Ligand | BDBM404910 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2022793 (CHEMBL4676606) |
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IC50 | 32±n/a nM |
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Citation | Soth, MJ; Le, K; Di Francesco, ME; Hamilton, MM; Liu, G; Burke, JP; Carroll, CL; Kovacs, JJ; Bardenhagen, JP; Bristow, CA; Cardozo, M; Czako, B; de Stanchina, E; Feng, N; Garvey, JR; Gay, JP; Do, MKG; Greer, J; Han, M; Harris, A; Herrera, Z; Huang, S; Giuliani, V; Jiang, Y; Johnson, SB; Johnson, TA; Kang, Z; Leonard, PG; Liu, Z; McAfoos, T; Miller, M; Morlacchi, P; Mullinax, RA; Palmer, WS; Pang, J; Rogers, N; Rudin, CM; Shepard, HE; Spencer, ND; Theroff, J; Wu, Q; Xu, A; Yau, JA; Draetta, G; Toniatti, C; Heffernan, TP; Jones, P Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties. J Med Chem63:12957-12977 (2020) [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 |
Synonyms: | GLS | GLS1 | GLSK_HUMAN | Glutaminase 1 | K-glutaminase | KIAA0838 | L-glutamine amidohydrolase |
Type: | Protein |
Mol. Mass.: | 73471.89 |
Organism: | Homo sapiens (Human) |
Description: | O94925 |
Residue: | 669 |
Sequence: | MMRLRGSGMLRDLLLRSPAGVSATLRRAQPLVTLCRRPRGGGRPAAGPAAAARLHPWWGG
GGWPAEPLARGLSSSPSEILQELGKGSTHPQPGVSPPAAPAAPGPKDGPGETDAFGNSEG
KELVASGENKIKQGLLPSLEDLLFYTIAEGQEKIPVHKFITALKSTGLRTSDPRLKECMD
MLRLTLQTTSDGVMLDKDLFKKCVQSNIVLLTQAFRRKFVIPDFMSFTSHIDELYESAKK
QSGGKVADYIPQLAKFSPDLWGVSVCTVDGQRHSTGDTKVPFCLQSCVKPLKYAIAVNDL
GTEYVHRYVGKEPSGLRFNKLFLNEDDKPHNPMVNAGAIVVTSLIKQGVNNAEKFDYVMQ
FLNKMAGNEYVGFSNATFQSERESGDRNFAIGYYLKEKKCFPEGTDMVGILDFYFQLCSI
EVTCESASVMAATLANGGFCPITGERVLSPEAVRNTLSLMHSCGMYDFSGQFAFHVGLPA
KSGVAGGILLVVPNVMGMMCWSPPLDKMGNSVKGIHFCHDLVSLCNFHNYDNLRHFAKKL
DPRREGGDQRVKSVINLLFAAYTGDVSALRRFALSAMDMEQRDYDSRTALHVAAAEGHVE
VVKFLLEACKVNPFPKDRWNNTPMDEALHFGHHDVFKILQEYQVQYTPQGDSDNGKENQT
VHKNLDGLL
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BDBM404910 |
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n/a |
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Name | BDBM404910 |
Synonyms: | (R)-1-(2-fluoro-4-(6-(2-(pyridin-2- yl)acetamido)pyridazin-3-yl)butyl)- N-methyl-1H-1,2,3-triazole-4- carboxamide | US10344025, Example 254 | US11370786, Example 254 |
Type | Small organic molecule |
Emp. Form. | C19H21FN8O2 |
Mol. Mass. | 412.4208 |
SMILES | CNC(=O)c1cn(C[C@H](F)CCc2ccc(NC(=O)Cc3ccccn3)nn2)nn1 |r| |
Structure |
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