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TargetGlutaminase kidney isoform, mitochondrial
LigandBDBM404825
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2022793 (CHEMBL4676606)
IC50 6.0±n/a nM
Citation Soth, MJLe, KDi Francesco, MEHamilton, MMLiu, GBurke, JPCarroll, CLKovacs, JJBardenhagen, JPBristow, CACardozo, MCzako, Bde Stanchina, EFeng, NGarvey, JRGay, JPDo, MKGGreer, JHan, MHarris, AHerrera, ZHuang, SGiuliani, VJiang, YJohnson, SBJohnson, TAKang, ZLeonard, PGLiu, ZMcAfoos, TMiller, MMorlacchi, PMullinax, RAPalmer, WSPang, JRogers, NRudin, CMShepard, HESpencer, NDTheroff, JWu, QXu, AYau, JADraetta, GToniatti, CHeffernan, TPJones, 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
More Info.:Get all data from this article,  Assay Method
 
Glutaminase kidney isoform, mitochondrial
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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  Blast E-value cutoff:
BDBM404825
n/a
NameBDBM404825
Synonyms:1-(4-{6-[2-(pyridin-2- yl)acetamido]pyridazin-3-yl}butyl)- N-{[3-(trifluoromethoxy)phenyl] methyl}-1H-1,2,3-triazole-4- carboxamide | US10344025, Example 169 | US11370786, Example 169
TypeSmall organic molecule
Emp. Form.C26H25F3N8O3
Mol. Mass.554.5237
SMILESFC(F)(F)Oc1cccc(CNC(=O)c2cn(CCCCc3ccc(NC(=O)Cc4ccccn4)nn3)nn2)c1
Structure
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