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Assay Detail

CHEMBL933109

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]PGE4 from human EP4 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin E2 receptor EP4 subtype (CHEMBL1836)
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
Ki 11 8.74 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258332 1 10.70
CHEMBL272276 1 10.30
CHEMBL548 DINOPROSTONE 4.0 1 9.10
CHEMBL251294 1 9.00
CHEMBL257217 1 9.00
CHEMBL222715 1 8.70
CHEMBL272277 1 8.70
CHEMBL257658 1 8.05
CHEMBL271488 1 7.57
CHEMBL272969 1 6.31
CHEMBL271896 BUTAPROST 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258332 Ki = 0.02 nM 10.70
CHEMBL272276 Ki = 0.05 nM 10.30
CHEMBL548 DINOPROSTONE Ki = 0.79 nM 9.10
CHEMBL251294 Ki = 1.0 nM 9.00
CHEMBL257217 Ki = 1.0 nM 9.00
CHEMBL222715 Ki = 2.0 nM 8.70
CHEMBL272277 Ki = 2.0 nM 8.70
CHEMBL257658 Ki = 9.0 nM 8.05
CHEMBL271488 Ki = 27.0 nM 7.57
CHEMBL272969 Ki = 490.0 nM 6.31
CHEMBL271896 BUTAPROST Ki > 10000.0 nM -