ONO-8430506

ONO-8430506 : Inhibitor of ENPP2

Structure

SERP Rating

In Cells

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In Model Organisms

(1 ratings)

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Probe ONO-8430506 is in the process of SERP review.

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Information

ENPP2

Inhibitor

In Vitro Validations

Uniprot ID: Q13822

Target Class: Enzyme

Target SubClass: nucleotide pyrophosphatase/phosphodiesterase; lysophospholipase

Potency: IC50

Potency Value: 5.1 nM

Potency Assay: LysoPLD activity of recombinant human ATX/ENPP2 using synthetic fluorescent substrate FS-3 after 2h

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Autotaxin, PDNP2, ATX, ENPP2, ENPP2_HUMAN, LysoPLD ...

DOI Reference: 10.1371/journal.pone.0093230

Uniprot ID: Q13822

Target Class: Enzyme

Target SubClass: nucleotide pyrophosphatase/phosphodiesterase; lysophospholipase

Potency: IC50

Potency Value: 4.5 nM

Potency Assay: LysoPLD activity of recombinant human ATX/ENPP2 using natural substrate 16:0-LPC after 30 min

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Autotaxin, PDNP2, ATX, ENPP2, ENPP2_HUMAN, LysoPLD ...

DOI Reference: 10.1371/journal.pone.0093230

Uniprot ID: Q13822

Target Class: Enzyme

Target SubClass: nucleotide pyrophosphatase/phosphodiesterase; lysophospholipase

Potency: IC50

Potency Value: 20-30 nM

Potency Assay: inhibition of lysophosphatidic acid (LPA) formation in human plasma

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Autotaxin, PDNP2, ATX, ENPP2, ENPP2_HUMAN, LysoPLD ...

DOI Reference: 10.1371/journal.pone.0093230

In Cell Validations

No in Cell Validations available

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): ONO-8430506 was proved to be a selective inhibitor of ATX/ENPP2 as the compound showed no inhibition of other two ENPP family enzymes, ENPP4 of which substrate is a nucleic acid and ENPP6 of which substrate is glycerophosphorylcholine, up to 100 µM. Further, the compound showed no inhibition of radioligand-binding to other approximately sixty pharmacological drug targets, such as neurotransmitter receptors, ion channels and transporters, at 10 µM.

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SERP ratings and comments

SERP Ratings

In Model Organisms

SERP Comments:

ONO-8430506 is a potent and selective inhibitor of ENPP2 (also known as Autotaxin, ATX). It shows robust PD activity in rat (inhibition of LPA formation in plasma), and regulates urethral tension in a rat model. It also enhances the antitumour activity of paclitaxel in a mouse breast cancer model. ONO-8430506 is a quality compound for the investigation of the role of ENPP2 in in vitro and in vivo models.

(last updated: 16 Apr 2025 )