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Assay Detail

CHEMBL618238

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

Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS-7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.
Chang-Fong J, Rangisetty JB, Dukat M, Setola V, Raffay T, Roth B, Glennon RA.
Bioorg Med Chem Lett (2004) 14 : 1961 -1964
PubMed 15050637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.51 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353552 1 9.52
CHEMBL175068 1 8.70
CHEMBL92093 1 8.64
CHEMBL366935 1 8.62
CHEMBL368746 1 8.30
CHEMBL177107 1 8.29
CHEMBL425328 1 8.12
CHEMBL178691 1 8.03
CHEMBL435524 1 7.85
CHEMBL1189868 1 7.54
CHEMBL368294 1 7.33
CHEMBL2113365 1 7.31
CHEMBL435534 1 7.19
CHEMBL329046 1 6.87
CHEMBL7228 1 6.78
CHEMBL368132 1 6.70
CHEMBL176838 1 6.52
CHEMBL368783 1 5.22
CHEMBL177233 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353552 Ki = 0.3 nM 9.52
CHEMBL175068 Ki = 2.0 nM 8.70
CHEMBL92093 Ki = 2.3 nM 8.64
CHEMBL366935 Ki = 2.4 nM 8.62
CHEMBL368746 Ki = 5.0 nM 8.30
CHEMBL177107 Ki = 5.1 nM 8.29
CHEMBL425328 Ki = 7.6 nM 8.12
CHEMBL178691 Ki = 9.4 nM 8.03
CHEMBL435524 Ki = 14.0 nM 7.85
CHEMBL1189868 Ki = 29.0 nM 7.54
CHEMBL368294 Ki = 47.0 nM 7.33
CHEMBL2113365 Ki = 49.0 nM 7.31
CHEMBL435534 Ki = 64.0 nM 7.19
CHEMBL329046 Ki = 136.0 nM 6.87
CHEMBL7228 Ki = 168.0 nM 6.78
CHEMBL368132 Ki = 200.0 nM 6.70
CHEMBL176838 Ki = 300.0 nM 6.52
CHEMBL368783 Ki = 6000.0 nM 5.22
CHEMBL177233 Ki = 6000.0 nM 5.22