BAY-6672 | Antagonist of PTGFR
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PTGFR
  • IC50:22 nM
  • Ki:16 nM
  • IC50:11 nM
  • IC50:12-18 nM
  • IC50:52 nM
Antagonist
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
> 420-fold selectivity vs prostanoids EP1–EP4, IP, DP, CRTH2 based on binding assays (Panlabs) Outs ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
hTP-R cell-based assay at Panlabs shows 200 fold selectivity in Cell-Based assay.

Potency
Cellular
In Vitro

PTGFR

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c00834

In Vivo Validations

Mouse, Rat, Dog
Dose: 3-30 mg/Kg
Route of delivery: Oral
Plasma half life: 3.4 (M), 3.8 (R), 14 (D) h

DOI Reference: 10.1021/acs.jmedchem.0c00834

Negative Control Compounds

BAY-403

Chemical Information

Molecular Formula C26H27BrClN3O3
SMILEs Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl
InChI InChI=1S/C26H27BrClN3O3/c1-16-24(20-14-18(27)9-10-22(20)30-25(16)31-12-4-5-13-31)26(34)29-15-17(8-11-23(32)33)19-6-2-3-7-21(19)28/h2-3,6-7,9-10,14,17H,4-5,8,11-13,15H2,1H3,(H,29,34)(H,32,33)/t17-/m0/s1
Molecular weight 543.09 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 61

Vendors

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Expert Reviews


(on 10 Apr 2021 )
Cellular Use Rating
In Model Organisms
BAY-6672 is a potent, selective and well-characterised antagonist of the prostaglandin FP receptor, suitable for use in vitro and in vivo.
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