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Assay Detail

CHEMBL4326151

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

Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 36 7.67 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3707245 OMIDENEPAG 2.0 1 8.96
CHEMBL4467099 1 8.80
CHEMBL4471378 1 8.70
CHEMBL4515583 1 8.59
CHEMBL4466224 1 8.57
CHEMBL4442505 1 8.57
CHEMBL4591201 1 8.55
CHEMBL4476670 1 8.47
CHEMBL4456588 1 8.37
CHEMBL4447271 1 8.36
CHEMBL4458330 1 8.35
CHEMBL4470479 1 8.25
CHEMBL4587628 1 8.21
CHEMBL4594090 1 7.89
CHEMBL2105672 EVATANEPAG SODIUM -1.0 1 7.77
CHEMBL4462507 1 7.75
CHEMBL4548451 1 7.72
CHEMBL4466523 1 7.54
CHEMBL4449902 1 7.46
CHEMBL4449855 1 7.37
CHEMBL4561017 1 7.35
CHEMBL4531171 1 7.12
CHEMBL4451941 1 7.08
CHEMBL4554216 1 7.04
CHEMBL4566584 1 6.96
CHEMBL4539881 1 6.93
CHEMBL4451786 1 6.92
CHEMBL4519118 1 6.55
CHEMBL4473407 1 6.51
CHEMBL4521659 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3707245 OMIDENEPAG EC50 = 1.1 nM 8.96
CHEMBL4467099 EC50 = 1.6 nM 8.80
CHEMBL4471378 EC50 = 2.0 nM 8.70
CHEMBL4515583 EC50 = 2.6 nM 8.59
CHEMBL4466224 EC50 = 2.7 nM 8.57
CHEMBL4442505 EC50 = 2.7 nM 8.57
CHEMBL4591201 EC50 = 2.8 nM 8.55
CHEMBL4476670 EC50 = 3.4 nM 8.47
CHEMBL4456588 EC50 = 4.3 nM 8.37
CHEMBL4447271 EC50 = 4.4 nM 8.36
CHEMBL4458330 EC50 = 4.5 nM 8.35
CHEMBL4470479 EC50 = 5.6 nM 8.25
CHEMBL4587628 EC50 = 6.1 nM 8.21
CHEMBL4594090 EC50 = 13.0 nM 7.89
CHEMBL2105672 EVATANEPAG SODIUM EC50 = 17.0 nM 7.77
CHEMBL4462507 EC50 = 18.0 nM 7.75
CHEMBL4548451 EC50 = 19.0 nM 7.72
CHEMBL4466523 EC50 = 29.0 nM 7.54
CHEMBL4449902 EC50 = 35.0 nM 7.46
CHEMBL4449855 EC50 = 43.0 nM 7.37
CHEMBL4561017 EC50 = 45.0 nM 7.35
CHEMBL4531171 EC50 = 75.0 nM 7.12
CHEMBL4451941 EC50 = 83.0 nM 7.08
CHEMBL4554216 EC50 = 91.0 nM 7.04
CHEMBL4566584 EC50 = 109.0 nM 6.96
CHEMBL4539881 EC50 = 118.0 nM 6.93
CHEMBL4451786 EC50 = 119.0 nM 6.92
CHEMBL4519118 EC50 = 283.0 nM 6.55
CHEMBL4473407 EC50 = 307.0 nM 6.51
CHEMBL4521659 EC50 = 360.0 nM 6.44
CHEMBL4460294 EC50 = 620.0 nM 6.21
CHEMBL4514124 EC50 = 649.0 nM 6.19
CHEMBL4527224 EC50 > 1000.0 nM -
CHEMBL4593898 EC50 > 1000.0 nM -
CHEMBL4586861 EC50 > 1000.0 nM -
CHEMBL4467297 EC50 > 1000.0 nM -