BAY-6672

Antagonist of PTGFR

Structure

Information

  • PTGFR
  • Antagonist
  • up to 500 nM

In Vitro Validations

Uniprot ID: P43088
Target Class: GPCR
Target SubClass: Prostaglandin F Receptor
Potency: IC50
Potency Value: 22 nM
Potency Assay: Panlabs binding assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Prostaglandin F2-alpha receptor, PTGFR, PF2R_HUMAN ...

DOI Reference: 10.1021/acs.jmedchem.0c00834

Uniprot ID: P43088
Target Class: GPCR
Target SubClass: Prostaglandin F Receptor
Potency: Ki
Potency Value: 16 nM
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Prostaglandin F2-alpha receptor, PTGFR, PF2R_HUMAN ...

DOI Reference: 10.1021/acs.jmedchem.0c00834

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
> 420-fold selectivity vs prostanoids EP1–EP4, IP, DP, CRTH2 based on binding assays (Panlabs) Outside Target Family: In a lead profiling screen comprising a broad range of more than 80 targets, including GPCRs, ion channels, nuclear hormone receptors, and other proteins and enzymes, no significant findings were noted at concentrations of 10 μM (Panlabs).
Probe Selectivity in Cell:
hTP-R cell-based assay at Panlabs shows 200 fold selectivity in Cell-Based assay.
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

BAY-6672 is a potent, selective and well-characterised antagonist of the prostaglandin FP receptor, suitable for use in vitro and in vivo.

(last updated: 10 Apr 2021 )