BAY-386

BAY-386 : Antagonist of F2R

Structure

SERP Rating

In Cells

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Probe BAY-386 is in the process of SERP review.

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Information

Antagonist

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P25116

Target Class: GPCR

Target SubClass: Trombin Receptor

Potency: IC50

Potency Value: 56 nM

Potency Assay: Binding assay (platelet membranes)

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

Target aliases:

Proteinase-activated receptor 1, TR, PAR1, CF2R, F ...

DOI Reference: 10.7554/eLife.34311

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: F2RL3 (PAR4): Functional cellular assay (HEK cells) IC50 > 10 µM ( > 1,000 fold selectivity) Eurofins-Cerep cellular and nuclear receptor functional assay screen (25) at 10 µM: Closest off-target: CNR1 (80.7 % Inhibition of control agonist response). CNR1 functional test (GTPγS binding): IC50 = 10.6 µM Eurofins-Panlabs radioligand binding assay (68) at 10 µM: Closest hit: CNR1 (88 % inhibition). One hit in the GPCR scan: TMEM97 (pKi = 5.94). Selectivity outside target family: Eurofins-Panlabs radioligand binding assay (68) at 10 µM: Closest hit outside the GPCR family is the Sarcolemmal Na+ channel site 2 (55 % inhibition).

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(last updated: 28 Jun 2022 )