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Assay Detail

CHEMBL911322

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

Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
8
Total Activities
8
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

Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors.
Kolanos R, Dukat M, Roth BL, Glennon RA.
Bioorg Med Chem Lett (2006) 16 : 5832 -5835
PubMed 16945532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.12 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220566 1 7.96
CHEMBL7257 MEBUFOTENIN 2.0 1 7.89
CHEMBL385330 1 7.85
CHEMBL223637 1 7.82
CHEMBL426567 1 6.97
CHEMBL375594 1 6.84
CHEMBL142936 DIETHYLTRYPTAMINE 1 6.24
CHEMBL3706857 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220566 Ki = 11.0 nM 7.96
CHEMBL7257 MEBUFOTENIN Ki = 13.0 nM 7.89
CHEMBL385330 Ki = 14.0 nM 7.85
CHEMBL223637 Ki = 15.0 nM 7.82
CHEMBL426567 Ki = 106.0 nM 6.97
CHEMBL375594 Ki = 143.0 nM 6.84
CHEMBL142936 DIETHYLTRYPTAMINE Ki = 575.0 nM 6.24
CHEMBL3706857 Ki = 4500.0 nM 5.35