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Assay Detail

CHEMBL4326150

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

Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.
Iwamura R, Tanaka M, Okanari E, Kirihara T, Odani-Kawabata N, Shams N, Yoneda K.
J Med Chem (2018) 61 : 6869 -6891
PubMed 29995405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.33 7.82
IC50 3 7.26 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL548 DINOPROSTONE 4.0 1 8.40
CHEMBL3707245 OMIDENEPAG 2.0 1 8.00
CHEMBL4443289 1 7.82
CHEMBL2105672 EVATANEPAG SODIUM -1.0 1 7.80
CHEMBL4448995 1 6.36
CHEMBL4297666 OMIDENEPAG ISOPROPYL 4.0 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL548 DINOPROSTONE IC50 = 4.0 nM 8.40
CHEMBL3707245 OMIDENEPAG IC50 = 10.0 nM 8.00
CHEMBL4443289 Ki = 15.0 nM 7.82
CHEMBL2105672 EVATANEPAG SODIUM Ki = 16.0 nM 7.80
CHEMBL4448995 Ki = 433.0 nM 6.36
CHEMBL4297666 OMIDENEPAG ISOPROPYL IC50 = 4180.0 nM 5.38