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Assay Detail

CHEMBL2188200

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

Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assay
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.
Dubost E, Dumas N, Fossey C, Magnelli R, Butt-Gueulle S, Ballandonne C, Caignard DH, Dulin F, Sopkova de-Oliveira Santos J, Millet P, Charnay Y, Rault S, Cailly T, Fabis F.
J Med Chem (2012) 55 : 9693 -9707
PubMed 23102207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.79 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181170 2 10.40
CHEMBL2181166 1 9.64
CHEMBL2181168 1 9.59
CHEMBL2181169 1 8.92
CHEMBL2181167 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181170 Ki = 0.03981 nM 10.40
CHEMBL2181170 Ki = 0.04 nM 10.40
CHEMBL2181166 Ki = 0.23 nM 9.64
CHEMBL2181168 Ki = 0.26 nM 9.59
CHEMBL2181169 Ki = 1.2 nM 8.92
CHEMBL2181167 Ki - -