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ZIRITAXESTAT

ZIRITAXESTAT : LPC competitive inhibitor of ENPP2

Structure

Information

  • ENPP2
  • LPC competitive
  • up to 1 uM

In Vitro Validations

Uniprot ID: Q13822
Target Class: Enzyme
Target SubClass: pyrophosphatase/phosphodiesterase
Potency: Ki
Potency Value: 15 nM
Potency Assay: Human ATX biochemical assay using LPC 16:0 as substrate.
PDB ID for probe-target interaction (3D structure): 5MHP
Target aliases:
Ectonucleotide pyrophosphatase/phosphodiesterase f ...

DOI Reference: 10.1021/acs.jmedchem.7b00032

Uniprot ID: Q13822
Target Class: Enzyme
Target SubClass: pyrophosphatase/phosphodiesterase
Potency: IC50
Potency Value: 131 nM
Potency Assay: biochemical assays with human enzyme
PDB ID for probe-target interaction (3D structure): 5MHP
Target aliases:
Ectonucleotide pyrophosphatase/phosphodiesterase f ...

DOI Reference: 10.1021/acs.jmedchem.7b00032

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): The compound was selective over related enzymes like ENPP1, phosphodiesterase 4 (PDE4) and PDE5 (enzymes with phosphodiesterase activity), and phospholipase A (PLA) or phospholipase C (PLC) (enzymes with phospholipase A or C activity, respectively). Moreover, GLPG1690 showed no inhibition in a panel of kinases. In a Cerep diversity panel (98 targets including receptors and ion channels), only 3 targets displayed more than 50% inhibition at 10 µM. (published on: Clinical Study Protocol GLPG1690-CL-202)
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