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Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM405076
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
<100±n/a nM
Citation
 Di Francesco, ME; Jones, P; Heffernan, T; Hamilton, MM; Kang, Z; Soth, MJ; Burke, JP; Le, K; Carroll, CL; Palmer, WS; Lewis, R; McAfoos, T; Czako, B; Liu, G; Theroff, J; Herrera, Z; Yau, A GLS1 inhibitors for treating disease US Patent  US10344025 Publication Date 7/9/2019 
Target
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:
MMRLRGSGMLRDLLLRSPAGVSATLRRAQPLVTLCRRPRGGGRPAAGPAAAARLHPWWGGGGWPAEPLARGLSSSPSEILQELGKGSTHPQPGVSPPAAPAAPGPKDGPGETDAFGNSEGKELVASGENKIKQGLLPSLEDLLFYTIAEGQEKIPVHKFITALKSTGLRTSDPRLKECMDMLRLTLQTTSDGVMLDKDLFKKCVQSNIVLLTQAFRRKFVIPDFMSFTSHIDELYESAKKQSGGKVADYIPQLAKFSPDLWGVSVCTVDGQRHSTGDTKVPFCLQSCVKPLKYAIAVNDLGTEYVHRYVGKEPSGLRFNKLFLNEDDKPHNPMVNAGAIVVTSLIKQGVNNAEKFDYVMQFLNKMAGNEYVGFSNATFQSERESGDRNFAIGYYLKEKKCFPEGTDMVGILDFYFQLCSIEVTCESASVMAATLANGGFCPITGERVLSPEAVRNTLSLMHSCGMYDFSGQFAFHVGLPAKSGVAGGILLVVPNVMGMMCWSPPLDKMGNSVKGIHFCHDLVSLCNFHNYDNLRHFAKKLDPRREGGDQRVKSVINLLFAAYTGDVSALRRFALSAMDMEQRDYDSRTALHVAAAEGHVEVVKFLLEACKVNPFPKDRWNNTPMDEALHFGHHDVFKILQEYQVQYTPQGDSDNGKENQTVHKNLDGLL
  
Inhibitor
Name:
BDBM405076
Synonyms:
5-[3-fluoro-4-(4-{[(6-methylpyridin- 3-yl)methyl]carbamoyl}-1H-1,2,3- triazol-1-yl)butyl]-N-{[3- (trifluoromethoxy)phenyl]methyl}- 1,3,4-thiadiazole-2-carboxamide | US10344025, Example 420 | US11370786, Example 420
Type:
Small organic molecule
Emp. Form.:
C25H24F4N8O3S
Mol. Mass.:
592.568
SMILES:
Cc1ccc(CNC(=O)c2cn(CC(F)CCc3nnc(s3)C(=O)NCc3cccc(OC(F)(F)F)c3)nn2)cn1
Structure:
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