IMR-687

Inhibitor of PDE9A

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe IMR-687 is in the process of SERP review.

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Information

PDE9A

Inhibitor

up to 10 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O76083

Target Class: Nucleic acid metabolism

Target SubClass: Phosphodiesterase

Potency: IC50

Potency Value: 9 nM

Potency Assay: Phosphodiesterase enzyme (PDE) inhibition IC50 values were determined for IMR-687 using recombinant human PDE enzymes in a radiometric assay

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

Target aliases:

High affinity cGMP-specific 3',5'-cyclic phosphodi ...

DOI Reference: 10.3324/haematol.2018.213462

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Radiometric assay

Probe Selectivity in Vitro:

MR-687 inhibited PDE9A with more than 800-fold greater potency than PDE1A3, PDE1B, PDE1C, PDE5A2, with IC50 values of 88.4 μM, 8.48 μM, 12.2 μM, and 81.9 μM, respectively. Significant inhibition of the other 27 PDE enzymes tested, including PDE4 and PDE10, was not observed.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

IMR-687 was tested against 33 PDEs and shows 800 fold selectivity against PDE9A1 and PDE9A2. However, specific in-cell data (e.g. target engagement) is missing to fully evaluate it as a cellular probe.

(last updated: 22 Mar 2023 )