Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM404691
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  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:
BDBM404691
Synonyms:
N-benzyl-5-(4-{6-[2-(pyridin-3- yl)acetamido]pyridazin-3-yl} butyl)-1,3,4-thiadiazole-2- carboxamide | US10344025, Example 30 | US11370786, Example 30
Type:
Small organic molecule
Emp. Form.:
C25H25N7O2S
Mol. Mass.:
487.577
SMILES:
O=C(Cc1cccnc1)Nc1ccc(CCCCc2nnc(s2)C(=O)NCc2ccccc2)nn1
Structure:
Search PDB for entries with ligand similarity: