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Assay Detail

CHEMBL859603

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

Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.
Becker DP, Flynn DL, Moormann AE, Nosal R, Villamil CI, Loeffler R, Gullikson GW, Moummi C, Yang DC.
J Med Chem (2006) 49 : 1125 -1139
PubMed 16451077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.83 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201946 1 9.74
CHEMBL201621 1 9.74
CHEMBL199866 1 9.46
CHEMBL383577 1 9.40
CHEMBL202122 1 9.15
CHEMBL201878 1 9.10
CHEMBL202434 1 8.85
CHEMBL34291 1 8.28
CHEMBL201414 1 8.15
CHEMBL1729 CISAPRIDE 4.0 1 7.77
CHEMBL2448165 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201946 Ki = 0.183 nM 9.74
CHEMBL201621 Ki = 0.183 nM 9.74
CHEMBL199866 Ki = 0.35 nM 9.46
CHEMBL383577 Ki = 0.4 nM 9.40
CHEMBL202122 Ki = 0.7 nM 9.15
CHEMBL201878 Ki = 0.8 nM 9.10
CHEMBL202434 Ki = 1.4 nM 8.85
CHEMBL34291 Ki = 5.2 nM 8.28
CHEMBL201414 Ki = 7.0 nM 8.15
CHEMBL1729 CISAPRIDE Ki = 17.0 nM 7.77
CHEMBL2448165 Ki = 29.0 nM 7.54