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Assay Detail

CHEMBL3757318

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Binding
Agonist activity at human EP3 receptor
12
Total Activities
12
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 EP3 subtype (CHEMBL3710)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of highly potent dual EP(2) and EP(3) agonists with subtype selectivity.
Kinoshita A, Higashino M, Aratani Y, Kakuuchi A, Matsuya H, Ohmoto K.
Bioorg Med Chem Lett (2016) 26 : 1016 -1019
PubMed 26725951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.62 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753221 1 8.41
CHEMBL3752406 1 8.33
CHEMBL3752435 1 8.17
CHEMBL3754197 1 8.13
CHEMBL3752377 1 8.08
CHEMBL3751951 1 8.00
CHEMBL3753268 1 7.75
CHEMBL3753788 1 7.60
CHEMBL3753622 1 7.57
CHEMBL3753853 1 7.30
CHEMBL3754586 1 6.51
CHEMBL3753898 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753221 EC50 = 3.9 nM 8.41
CHEMBL3752406 EC50 = 4.7 nM 8.33
CHEMBL3752435 EC50 = 6.7 nM 8.17
CHEMBL3754197 EC50 = 7.4 nM 8.13
CHEMBL3752377 EC50 = 8.4 nM 8.08
CHEMBL3751951 EC50 = 10.0 nM 8.00
CHEMBL3753268 EC50 = 18.0 nM 7.75
CHEMBL3753788 EC50 = 25.0 nM 7.60
CHEMBL3753622 EC50 = 27.0 nM 7.57
CHEMBL3753853 EC50 = 50.0 nM 7.30
CHEMBL3754586 EC50 = 310.0 nM 6.51
CHEMBL3753898 EC50 = 2606.0 nM 5.58