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Assay Detail

CHEMBL620782

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

Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
Riemer C, Borroni E, Levet-Trafit B, Martin JR, Poli S, Porter RH, Bös M.
J Med Chem (2003) 46 : 1273 -1276
PubMed 12646038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.25 9.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24474 1 9.94
CHEMBL23038 1 9.00
CHEMBL23575 1 8.64
CHEMBL23965 1 7.37
CHEMBL415464 1 7.27
CHEMBL542806 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24474 Ki = 0.1148 nM 9.94
CHEMBL23038 Ki = 1.0 nM 9.00
CHEMBL23575 Ki = 2.291 nM 8.64
CHEMBL23965 Ki = 42.66 nM 7.37
CHEMBL415464 Ki = 53.7 nM 7.27
CHEMBL542806 Ki = 54.95 nM 7.26