JNJ-65355394

JNJ-65355394 : Inhibitor of OGA

Structure

Information

  • OGA
  • Inhibitor
  • up to 1 uM

In Vitro Validations

Uniprot ID: O60502
Target Class: Enzyme
Target SubClass: Hydrolase
Potency: IC50
Potency Value: 1.3 nM
Potency Assay: Fluorescence-based enzymatic assay.
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein O-GlcNAcase, MGEA5, MEA5, KIAA0679, HEXC, ...

Other Reference: peer reviewed at SGC

Uniprot ID: O60502
Target Class: Enzyme
Target SubClass: Hydrolase
Potency: Ki
Potency Value: 0.035 nM
Potency Assay: Time dependent inhibition: t = 0 (Ki = 1.1 nM); t = 15 min (Ki = 0.035 nM). Kinetic profile: kinact = 0.0036 1/min; kinact/Ki = 3.27 1/(µM*s).
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein O-GlcNAcase, MGEA5, MEA5, KIAA0679, HEXC, ...

Other Reference: peer reviewed at SGC

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
Selectivity within target family: > 30-fold HEXA IC50 > 10 µM. Selectivity outside target family: CEREP panel (54 targets) at 10 µM: Closest hits are [% inhibition]: rat OPRK1 (78), rat ADORA2A (69); human OPRM1 (55).
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SERP ratings and comments


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