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Assay Detail

CHEMBL3794972

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Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural optimization and structure-functional selectivity relationship studies of G protein-biased EP2 receptor agonists.
Ogawa S, Watanabe T, Moriyuki K, Goto Y, Yamane S, Watanabe A, Tsuboi K, Kinoshita A, Okada T, Takeda H, Tani K, Maruyama T.
Bioorg Med Chem Lett (2016) 26 : 2446 -2449
PubMed 27055938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 8.69 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3794302 1 9.96
CHEMBL3793515 1 9.85
CHEMBL3794016 1 9.77
CHEMBL3793862 1 9.70
CHEMBL3792632 1 9.68
CHEMBL3793802 1 9.24
CHEMBL3794466 1 9.17
CHEMBL3793892 1 9.16
CHEMBL3793045 1 9.05
CHEMBL3794585 1 8.74
CHEMBL3793020 1 8.70
CHEMBL3794226 1 8.66
CHEMBL3793797 1 8.54
CHEMBL3793786 1 8.41
CHEMBL3793809 1 8.41
CHEMBL3793167 1 7.96
CHEMBL3793209 1 7.89
CHEMBL3793009 1 7.82
CHEMBL3793724 1 7.64
CHEMBL3792668 1 7.26
CHEMBL3794185 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3794302 EC50 = 0.11 nM 9.96
CHEMBL3793515 EC50 = 0.14 nM 9.85
CHEMBL3794016 EC50 = 0.17 nM 9.77
CHEMBL3793862 EC50 = 0.2 nM 9.70
CHEMBL3792632 EC50 = 0.21 nM 9.68
CHEMBL3793802 EC50 = 0.57 nM 9.24
CHEMBL3794466 EC50 = 0.68 nM 9.17
CHEMBL3793892 EC50 = 0.69 nM 9.16
CHEMBL3793045 EC50 = 0.9 nM 9.05
CHEMBL3794585 EC50 = 1.8 nM 8.74
CHEMBL3793020 EC50 = 2.0 nM 8.70
CHEMBL3794226 EC50 = 2.2 nM 8.66
CHEMBL3793797 EC50 = 2.9 nM 8.54
CHEMBL3793786 EC50 = 3.9 nM 8.41
CHEMBL3793809 EC50 = 3.9 nM 8.41
CHEMBL3793167 EC50 = 11.0 nM 7.96
CHEMBL3793209 EC50 = 13.0 nM 7.89
CHEMBL3793009 EC50 = 15.0 nM 7.82
CHEMBL3793724 EC50 = 23.0 nM 7.64
CHEMBL3792668 EC50 = 55.0 nM 7.26
CHEMBL3794185 EC50 = 114.0 nM 6.94