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Assay Detail

CHEMBL2447593

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

Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Acidic biphenyl derivatives: synthesis and biological activity of a new series of potent 5-HT(4) receptor antagonists.
Brudeli B, Andressen KW, Moltzau LR, Nilsen NO, Levy FO, Klaveness J.
Bioorg Med Chem (2013) 21 : 7134 -7145
PubMed 24113240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.80 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2440453 1 9.10
CHEMBL356359 PIBOSEROD 2.0 1 8.80
CHEMBL2440452 1 7.20
CHEMBL2440451 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2440453 Ki = 0.7943 nM 9.10
CHEMBL356359 PIBOSEROD Ki = 1.585 nM 8.80
CHEMBL2440452 Ki = 63.1 nM 7.20
CHEMBL2440451 Ki = 794.33 nM 6.10