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Assay Detail

CHEMBL2447590

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

Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

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 8 9.59 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33884 1 10.40
CHEMBL2440460 1 10.30
CHEMBL2440457 1 10.20
CHEMBL356359 PIBOSEROD 2.0 1 10.00
CHEMBL2440458 1 9.20
CHEMBL2440456 1 8.60
CHEMBL2440455 1 8.40
CHEMBL2440459 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33884 Ki = 0.03981 nM 10.40
CHEMBL2440460 Ki = 0.05012 nM 10.30
CHEMBL2440457 Ki = 0.0631 nM 10.20
CHEMBL356359 PIBOSEROD Ki = 0.1 nM 10.00
CHEMBL2440458 Ki = 0.631 nM 9.20
CHEMBL2440456 Ki = 2.512 nM 8.60
CHEMBL2440455 Ki = 3.981 nM 8.40
CHEMBL2440459 Ki = 0.001259 nM -