A-079

Antagonist of TRPA1

Structure

SERP Rating

Probe A-079 is in the process of SERP review.

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Information

TRPA1

Antagonist

1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: O75762

Target Class: Ion Channel

Target SubClass: Transient receptor, TRPV subfamily

Potency: IC50

Potency Value: 67 nM

Potency Assay: FLIPR-based Ca2+ assay.

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

Target aliases:

Transient receptor potential cation channel subfam ...

DOI Reference: 10.1016/j.pain.2011.01.049

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

A-967079 is >1000-fold selective over other TRP channels (TRPV1, TRPV3, TRPV4, or TRPM8). Outside target family: A-967079 is >150-fold selective over 75 tested proteins. In a CEREP panel of 75 enzymes, G-protein-coupled receptors, transporters, and ion channels A-967079 exhibited was modest inhibition on ligand binding to SLC6A3 (43%), SLC6A2 (32%), MTNR1A (31%), with no significant effects (<30%) on other 72 proteins. Shows off-target activity in the GPCR scan for SIGMAR1 (Ki = 505.48 nM)

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SERP ratings and comments

No SERP comments found for A-079