Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM404687
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:
BDBM404687
Synonyms:
5-{4-[6-(2-phenylacetamido) pyridazin-3-yl]butyl}-N-(2- phenylethyl)-1,3,4- thiadiazole-2-carboxamide | US10344025, Example 26 | US11370786, Example 26
Type:
Small organic molecule
Emp. Form.:
C27H28N6O2S
Mol. Mass.:
500.615
SMILES:
O=C(Cc1ccccc1)Nc1ccc(CCCCc2nnc(s2)C(=O)NCCc2ccccc2)nn1
Structure:
Search PDB for entries with ligand similarity: