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Assay Detail

CHEMBL2038097

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

Binding
Displacement of [3H]PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by scintillation counting
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP1 subtype (CHEMBL2181)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and evaluation of γ-lactam analogs of PGE₂ as EP4 and EP2/EP4 agonists.
Kambe T, Maruyama T, Nakai Y, Oida H, Maruyama T, Abe N, Nishiura A, Nakai H, Toda M.
Bioorg Med Chem (2012) 20 : 3502 -3522
PubMed 22546206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 5.56 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2037289 1 6.70
CHEMBL2037292 1 6.19
CHEMBL2036325 1 6.17
CHEMBL2036326 1 5.89
CHEMBL2036320 1 5.62
CHEMBL2036321 1 5.60
CHEMBL2036322 1 5.57
CHEMBL2037291 1 5.50
CHEMBL1957435 1 5.38
CHEMBL2036312 1 5.30
CHEMBL2036319 1 5.27
CHEMBL2036318 1 5.21
CHEMBL1957436 1 5.20
CHEMBL2036310 1 5.15
CHEMBL2037290 1 5.11
CHEMBL2036324 1 5.10
CHEMBL2036313 1 -
CHEMBL2036307 1 -
CHEMBL2036308 1 -
CHEMBL2036309 1 -
CHEMBL2036311 1 -
CHEMBL2036323 1 -
CHEMBL1933722 1 -
CHEMBL1957437 1 -
CHEMBL2036314 1 -
CHEMBL2036315 1 -
CHEMBL2036316 1 -
CHEMBL1933717 1 -
CHEMBL2036317 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2037289 Ki = 200.0 nM 6.70
CHEMBL2037292 Ki = 650.0 nM 6.19
CHEMBL2036325 Ki = 680.0 nM 6.17
CHEMBL2036326 Ki = 1300.0 nM 5.89
CHEMBL2036320 Ki = 2400.0 nM 5.62
CHEMBL2036321 Ki = 2500.0 nM 5.60
CHEMBL2036322 Ki = 2700.0 nM 5.57
CHEMBL2037291 Ki = 3200.0 nM 5.50
CHEMBL1957435 Ki = 4200.0 nM 5.38
CHEMBL2036312 Ki = 5000.0 nM 5.30
CHEMBL2036319 Ki = 5400.0 nM 5.27
CHEMBL2036318 Ki = 6100.0 nM 5.21
CHEMBL1957436 Ki = 6300.0 nM 5.20
CHEMBL2036310 Ki = 7100.0 nM 5.15
CHEMBL2037290 Ki = 7700.0 nM 5.11
CHEMBL2036324 Ki = 8000.0 nM 5.10
CHEMBL2036313 Ki > 10000.0 nM -
CHEMBL2036307 Ki > 10000.0 nM -
CHEMBL2036308 Ki > 10000.0 nM -
CHEMBL2036309 Ki > 10000.0 nM -
CHEMBL2036311 Ki > 10000.0 nM -
CHEMBL2036323 Ki > 10000.0 nM -
CHEMBL1933722 Ki > 10000.0 nM -
CHEMBL1957437 Ki > 10000.0 nM -
CHEMBL2036314 Ki > 10000.0 nM -
CHEMBL2036315 Ki > 10000.0 nM -
CHEMBL2036316 Ki > 10000.0 nM -
CHEMBL1933717 Ki > 10000.0 nM -
CHEMBL2036317 Ki > 10000.0 nM -