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Assay Detail

CHEMBL934144

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

Binding
Displacement of [3H]PGE2 from EP1 receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin E2 receptor EP1 subtype (CHEMBL1811)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel methylene-linked heterocyclic EP1 receptor antagonists.
Hall A, Bit RA, Brown SH, Chowdhury A, Giblin GM, Hurst DN, Kilford IR, Lewell X, Naylor A, Scoccitti T.
Bioorg Med Chem Lett (2008) 18 : 1592 -1597
PubMed 18262416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.46 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234940 1 8.60
CHEMBL403330 1 8.50
CHEMBL209800 1 8.30
CHEMBL272793 1 8.20
CHEMBL213221 1 8.20
CHEMBL255652 1 8.20
CHEMBL377852 1 8.10
CHEMBL255009 1 8.10
CHEMBL404525 1 8.00
CHEMBL270208 1 8.00
CHEMBL407175 1 8.00
CHEMBL207577 1 7.90
CHEMBL257464 1 7.70
CHEMBL401768 1 7.60
CHEMBL258057 1 7.60
CHEMBL403329 1 7.40
CHEMBL256674 1 7.40
CHEMBL408367 1 7.30
CHEMBL404760 1 7.30
CHEMBL403460 1 7.10
CHEMBL270174 1 6.80
CHEMBL403459 1 6.80
CHEMBL404239 1 6.50
CHEMBL535640 1 6.50
CHEMBL257846 1 6.20
CHEMBL258303 1 6.20
CHEMBL270162 1 6.20
CHEMBL273145 1 6.10
CHEMBL557194 1 -
CHEMBL538095 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234940 IC50 = 2.512 nM 8.60
CHEMBL403330 IC50 = 3.162 nM 8.50
CHEMBL209800 IC50 = 5.012 nM 8.30
CHEMBL272793 IC50 = 6.31 nM 8.20
CHEMBL213221 IC50 = 6.31 nM 8.20
CHEMBL255652 IC50 = 6.31 nM 8.20
CHEMBL377852 IC50 = 7.943 nM 8.10
CHEMBL255009 IC50 = 7.943 nM 8.10
CHEMBL404525 IC50 = 10.0 nM 8.00
CHEMBL270208 IC50 = 10.0 nM 8.00
CHEMBL407175 IC50 = 10.0 nM 8.00
CHEMBL207577 IC50 = 12.59 nM 7.90
CHEMBL257464 IC50 = 19.95 nM 7.70
CHEMBL401768 IC50 = 25.12 nM 7.60
CHEMBL258057 IC50 = 25.12 nM 7.60
CHEMBL403329 IC50 = 39.81 nM 7.40
CHEMBL256674 IC50 = 39.81 nM 7.40
CHEMBL408367 IC50 = 50.12 nM 7.30
CHEMBL404760 IC50 = 50.12 nM 7.30
CHEMBL403460 IC50 = 79.43 nM 7.10
CHEMBL270174 IC50 = 158.49 nM 6.80
CHEMBL403459 IC50 = 158.49 nM 6.80
CHEMBL404239 IC50 = 316.23 nM 6.50
CHEMBL535640 IC50 = 316.23 nM 6.50
CHEMBL257846 IC50 = 630.96 nM 6.20
CHEMBL258303 IC50 = 630.96 nM 6.20
CHEMBL270162 IC50 = 630.96 nM 6.20
CHEMBL273145 IC50 = 794.33 nM 6.10
CHEMBL557194 IC50 < 1000.0 nM -
CHEMBL538095 IC50 < 1000.0 nM -
CHEMBL258304 IC50 < 1000.0 nM -
CHEMBL270160 IC50 < 1000.0 nM -
CHEMBL269940 IC50 < 1000.0 nM -
CHEMBL403863 IC50 < 1000.0 nM -