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Assay Detail

CHEMBL618126

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

Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
14
Total Activities
13
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 Expert

Target

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

Publication

6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.
Isaac M, Slassi A, Xin T, MacLean N, Wilson J, McCallum K, Wang H, Demchyshyn L.
Bioorg Med Chem Lett (2000) 10 : 1719 -1721
PubMed 10937732 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.58 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46187 1 9.70
CHEMBL299822 2 9.22
CHEMBL416638 1 8.89
CHEMBL431298 1 8.89
CHEMBL298274 1 8.77
CHEMBL45977 1 8.52
CHEMBL47691 1 8.48
CHEMBL49598 1 8.44
CHEMBL45987 1 8.33
CHEMBL299569 1 8.31
CHEMBL45695 1 8.24
CHEMBL46071 1 7.90
CHEMBL433461 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46187 Ki = 0.2 nM 9.70
CHEMBL299822 Ki = 0.6 nM 9.22
CHEMBL299822 Ki = 0.8 nM 9.10
CHEMBL416638 Ki = 1.3 nM 8.89
CHEMBL431298 Ki = 1.3 nM 8.89
CHEMBL298274 Ki = 1.7 nM 8.77
CHEMBL45977 Ki = 3.0 nM 8.52
CHEMBL47691 Ki = 3.3 nM 8.48
CHEMBL49598 Ki = 3.6 nM 8.44
CHEMBL45987 Ki = 4.7 nM 8.33
CHEMBL299569 Ki = 4.9 nM 8.31
CHEMBL45695 Ki = 5.7 nM 8.24
CHEMBL46071 Ki = 12.6 nM 7.90
CHEMBL433461 Ki = 50.0 nM 7.30