Chemical Probes logo
PF-04418948 | Antagonist of PTGER2
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PTGER2
  • IC50:5 nM
Antagonist
< 300 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
No agonist activity is observed across the family. Clean GPCR scan.
Selectivity Assessment Description:
With the exception of LTB4R (960 fold), MT3 (104 fold) and PDE3A (700 fold), no significant off-targ ...

Potency
Cellular
In Vitro

PTGER2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1111/j.1476-5381.2011.01495.x

In Vivo Validations

Mouse
Dose: 0.1 - 10 mg/Kg
Route of delivery: Oral

DOI Reference: 10.1111/j.1476-5381.2011.01495.x

Rat
Dose: 1 - 10 mg/Kg
Route of delivery: Oral

DOI Reference: 10.1111/j.1476-5381.2011.01495.x

Negative Control Compounds

PF-04475866
Notes: Inhibition of binding to PTGER2: IC50 = 1.3 µM; clean in GPCR scan

Chemical Information

Molecular Formula C23H20FNO5
SMILEs COc1ccc2cc(OCC3(C(=O)O)CN(C(=O)c4ccc(F)cc4)C3)ccc2c1
InChI InChI=1S/C23H20FNO5/c1-29-19-8-4-17-11-20(9-5-16(17)10-19)30-14-23(22(27)28)12-25(13-23)21(26)15-2-6-18(24)7-3-15/h2-11H,12-14H2,1H3,(H,27,28)
Molecular weight 409.13 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 50

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

No SERP comments found for PF-04418948

Probe PF-04418948 is in the process of SERP review.

Please continue to check back for new reviews and commentary.