IMARADENANT

IMARADENANT : Antagonist of ADORA2A

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe IMARADENANT is in the process of SERP review.

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Information

ADORA2A

Antagonist

100 nM
Reviewer recommended concentration: up to 1 µM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within the target family: In radioligand binding competition assays AZD4635 is selective for A2AR against other adenosine receptors of 160 nM for A1 (selectivity of 94-fold), 64 nM for A2BR (selectivity of 37-fold) and >10 000 nM for A3 (selectivity >5882-fold).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Imaradenant (AZD 4635) appears to be a very good compound to probe the effects of A2A receptor signalling in vitro and in vivo. Publication of preclinical pharmacokinetic data and physical properties such as solubility would greatly enhance understanding of its potential wider use in cells and in vivo.

(last updated: 31 Oct 2022 )