LYS006

Inhibitor of LTA4H

Structure

Information

  • LTA4H
  • Inhibitor
  • up to 200 nM

In Vitro Validations

Uniprot ID: P09960
Target Class: Other
Target SubClass: Hydrolase
Potency: IC50
Potency Value: 0.12 nM
Potency Assay: LTA4H enzyme inhibition assay using Arg-AMC as substrate with <1 nM enzyme concentration
PDB ID for probe-target interaction (3D structure): 7AUZ
Structure-activity relationship: yes
Target aliases:
Leukotriene A-4 hydrolase, LTA4, LTA4H, LKHA4_HUMA ...

DOI Reference: 10.1021/acs.jmedchem.0c01955

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

LYS006 shows an exquisite selectivity profile when tested at concentrations of ≥10 μM in binding or functional mode on a panel of >150 GPCRs, transporters, ion channels, nuclear receptors, and enzymes in vitro. Inhibitory activity of LYS006 against selected Zn-containing enzymes showed no IC50 < 30 uM.

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