Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
ID: CHEMBL1143179
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Authors: Xiao Y, Araldi GL, Zhao Z, Reddy A, Karra S, Brugger N, Fischer D, Palmer E, Bao B, McKenna SD.
Abstract: Gamma-lactam analogs (2) of EP(4) receptor agonists were identified by substitution of the pyrazolidinone ring (1) with a pyrrolidinone ring. Several compounds (such as 2a, 2h) with high potency, selectivity and acceptable PK profiles were discovered. These were assessed in animal models of ovulation induction and bronchoconstriction.
CiteXplore: 18039575
Patent ID: ---
| ChEMBL ID | Target Similarity | Compound Similarity | Reference | Title | PubMed ID | DOI |
|---|---|---|---|---|---|---|
| CHEMBL1140010 | 0.86 | 0.1 | Bioorg Med Chem Lett (2007) 17:4323-4327 | Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists. | 17531488 | 10.1016/j.bmcl.2007.05.025 |
Protein Target Summary
Total
7
Eukaryotes
Assay Summary
Total
25
A - ADME
F - Functional
B - Binding
Bioactivity Summary
Total
66
Ki
EC50
ED50
AUC
Activity
T1/2
Tmax
F
CL
Drug uptake
Inhibition
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