Reaction Details Report a problem with these data
Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM405080
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
More Info.:
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:
BDBM405080
Synonyms:
1-{2-fluoro-4-[4-({[2-fluoro-5- (trifluoromethoxy)phenyl]methyl} carbamoyl)-1H-1,2,3-triazol-1-yl] butyl}-N-{[6-(trifluoromethyl) pyridin-3-yl]methyl}-1H-1,2,3- triazole-4-carboxamide | US10344025, Example 424 | US11370786, Example 424
Type:
Small organic molecule
Emp. Form.:
C25H21F8N9O3
Mol. Mass.:
647.48
SMILES:
FC(CCn1cc(nn1)C(=O)NCc1cc(OC(F)(F)F)ccc1F)Cn1cc(nn1)C(=O)NCc1ccc(nc1)C(F)(F)F