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Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM404721
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  US11370786 Publication Date 6/28/2022
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:
BDBM404721
Synonyms:
5-(4-{4-[(pyridin-2- ylmethyl)carbamoyl]-1H- 1,2,3-triazol-1-yl}butyl)-N-{[3- (trifluoromethoxy)phenyl]methyl}- 1,3,4-thiadiazole-2-carboxamide | US10344025, Example 65 | US11370786, Example 65
Type:
Small organic molecule
Emp. Form.:
C24H23F3N8O3S
Mol. Mass.:
560.551
SMILES:
FC(F)(F)Oc1cccc(CNC(=O)c2nnc(CCCCn3cc(nn3)C(=O)NCc3ccccn3)s2)c1
Structure:
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