Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM405098
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
<100±n/a nM
Citation
 Di Francesco, MEJones, PHeffernan, THamilton, MMKang, ZSoth, MJBurke, JPLe, KCarroll, CLPalmer, WSLewis, RMcAfoos, TCzako, BLiu, GTheroff, JHerrera, ZYau, 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:
BDBM405098
Synonyms:
5-{3-fluoro-4-[4-({[3- (trifluoromethoxy)phenyl]methyl} carbamoyl)-1H-1,2,3-triazol-1-yl] butyl}-N-[(6-methylpyridin-3-yl) methyl]-1,3,4-thiadiazole-2- carboxamide | US10344025, Example 442 | US11370786, Example 442
Type:
Small organic molecule
Emp. Form.:
C25H24F4N8O3S
Mol. Mass.:
592.568
SMILES:
Cc1ccc(CNC(=O)c2nnc(CCC(F)Cn3cc(nn3)C(=O)NCc3cccc(OC(F)(F)F)c3)s2)cn1
Structure:
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