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Assay Detail

CHEMBL3095863

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

Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL5017)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Design of fluorinated 5-HT(4)R antagonists: influence of the basicity and lipophilicity toward the 5-HT(4)R binding affinities.
Fontenelle CQ, Wang Z, Fossey C, Cailly T, Linclau B, Fabis F.
Bioorg Med Chem (2013) 21 : 7529 -7538
PubMed 24128816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.83 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181170 1 8.66
CHEMBL3093187 1 8.38
CHEMBL3093186 1 8.05
CHEMBL3093184 1 7.85
CHEMBL2181189 1 7.70
CHEMBL3093194 1 7.66
CHEMBL2177145 1 7.29
CHEMBL3093185 1 7.04
CHEMBL3093193 1 -
CHEMBL3093192 1 -
CHEMBL3093191 1 -
CHEMBL3093190 1 -
CHEMBL3093189 1 -
CHEMBL3093188 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181170 Ki = 2.2 nM 8.66
CHEMBL3093187 Ki = 4.2 nM 8.38
CHEMBL3093186 Ki = 9.0 nM 8.05
CHEMBL3093184 Ki = 14.1 nM 7.85
CHEMBL2181189 Ki = 20.1 nM 7.70
CHEMBL3093194 Ki = 22.0 nM 7.66
CHEMBL2177145 Ki = 51.5 nM 7.29
CHEMBL3093185 Ki = 91.4 nM 7.04
CHEMBL3093193 Ki - -
CHEMBL3093192 Ki - -
CHEMBL3093191 Ki - -
CHEMBL3093190 Ki - -
CHEMBL3093189 Ki - -
CHEMBL3093188 Ki - -