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Assay Detail

CHEMBL767811

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Binding
Binding affinity was determined against prostanoid EP3 receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prostaglandin E2 receptor EP3 subtype (CHEMBL3710)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.
Elworthy TR, Kertesz DJ, Kim W, Roepel MG, Quattrocchio-Setti L, Smith DB, Tracy JL, Chow A, Li F, Brill ER, Lach LK, McGee D, Yang DS, Chiou SS.
Bioorg Med Chem Lett (2004) 14 : 1655 -1659
PubMed 15026044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 5.02 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413509 1 8.10
CHEMBL42027 1 5.52
CHEMBL45418 1 5.31
CHEMBL440474 1 4.92
CHEMBL291182 1 4.92
CHEMBL45008 1 4.89
CHEMBL42129 1 4.80
CHEMBL280223 1 4.70
CHEMBL298026 1 4.42
CHEMBL46395 1 4.42
CHEMBL416262 1 4.25
CHEMBL14359 1 4.00
CHEMBL297578 1 -
CHEMBL296715 1 -
CHEMBL288978 1 -
CHEMBL417171 1 -
CHEMBL46671 1 -
CHEMBL444574 1 -
CHEMBL47138 1 -
CHEMBL47018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413509 Ki = 8.0 nM 8.10
CHEMBL42027 Ki = 3000.0 nM 5.52
CHEMBL45418 Ki = 4900.0 nM 5.31
CHEMBL440474 Ki = 12000.0 nM 4.92
CHEMBL291182 Ki = 12000.0 nM 4.92
CHEMBL45008 Ki = 13000.0 nM 4.89
CHEMBL42129 Ki = 16000.0 nM 4.80
CHEMBL280223 Ki = 20000.0 nM 4.70
CHEMBL298026 Ki = 38000.0 nM 4.42
CHEMBL46395 Ki = 38000.0 nM 4.42
CHEMBL416262 Ki = 56000.0 nM 4.25
CHEMBL14359 Ki = 100000.0 nM 4.00
CHEMBL297578 Ki > 100000.0 nM -
CHEMBL296715 Ki > 100000.0 nM -
CHEMBL288978 Ki > 100000.0 nM -
CHEMBL417171 Ki = 131000.0 nM -
CHEMBL46671 Ki > 100000.0 nM -
CHEMBL444574 Ki > 100000.0 nM -
CHEMBL47138 Ki > 100000.0 nM -
CHEMBL47018 Ki > 100000.0 nM -