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Assay Detail

CHEMBL931918

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Functional
Agonist activity at human EP2 receptor by cAMP assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP2 subtype (CHEMBL1881)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Xiao Y, Araldi GL, Zhao Z, Reddy A, Karra S, Brugger N, Fischer D, Palmer E, Bao B, McKenna SD.
Bioorg Med Chem Lett (2008) 18 : 821 -824
PubMed 18039575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.35 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272277 1 8.52
CHEMBL222715 1 7.82
CHEMBL257658 1 7.72
CHEMBL251294 1 7.10
CHEMBL258332 1 6.60
CHEMBL272276 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272277 EC50 = 3.0 nM 8.52
CHEMBL222715 EC50 = 15.0 nM 7.82
CHEMBL257658 EC50 = 19.0 nM 7.72
CHEMBL251294 EC50 = 80.0 nM 7.10
CHEMBL258332 EC50 = 250.0 nM 6.60
CHEMBL272276 EC50 = 434.0 nM 6.36