BMS-986235

BMS-986235 : Agonist of FPR2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(3 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.

Information

FPR2

Agonist

up to 100 nM
Reviewer recommended concentration: 100 nM to 1µM

Probe Availability:

MedChemExpress

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selective against FRP2 6800 fold

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Based on the public information there is no outside family selectivity data. Therefore, the users might also want to consider this point in interpreting the experimental outcomes. The indicated doses are from in vivo PK studies; however, the Cmax values with the given doses look like just around EC50 or below estimated from in vitro studies. Because there is no in vivo safety/tox data available it is hard to justify the maximal doses to be used in animal studies, but probably 10 mg/kg would be worthwhile to test with careful animal safety observation such as behaviour.

(last updated: 4 Mar 2024 )

SERP Ratings

In Model Organisms

(last updated: 17 Mar 2024 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

This is a highly potent FPR2 agonist with good selectivity against FPR1. However, no wider selectivity profiling beyond FPR1 and 2 have been provided. For cAMP biased signaling a dose no higher than 50nM is recommended. Thorough analysis of certain PK parameters including suitable Cmax and t1/2 are provided to support in vivo experiments. Yet plasma binding data, target engagement demonstrated in vivo and dose dependency measured in vivo has not been published.

(last updated: 14 Oct 2025 )