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Assay Detail

CHEMBL618124

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

Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S, Lee M, Glennon RA.
Bioorg Med Chem Lett (2000) 10 : 2295 -2299
PubMed 11055342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.05 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443796 1 9.05
CHEMBL75734 1 8.89
CHEMBL75010 1 8.80
CHEMBL76237 1 8.64
CHEMBL72574 1 8.51
CHEMBL42 CLOZAPINE 4.0 1 8.32
CHEMBL72554 1 8.30
CHEMBL75758 1 8.13
CHEMBL76466 1 8.10
CHEMBL419824 1 8.02
CHEMBL7257 MEBUFOTENIN 2.0 1 7.80
CHEMBL75029 1 7.35
CHEMBL39 SEROTONIN 3.0 1 7.11
CHEMBL74378 1 7.03
CHEMBL306569 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443796 Ki = 0.9 nM 9.05
CHEMBL75734 Ki = 1.3 nM 8.89
CHEMBL75010 Ki = 1.6 nM 8.80
CHEMBL76237 Ki = 2.3 nM 8.64
CHEMBL72574 Ki = 3.1 nM 8.51
CHEMBL42 CLOZAPINE Ki = 4.8 nM 8.32
CHEMBL72554 Ki = 5.0 nM 8.30
CHEMBL75758 Ki = 7.4 nM 8.13
CHEMBL76466 Ki = 8.0 nM 8.10
CHEMBL419824 Ki = 9.5 nM 8.02
CHEMBL7257 MEBUFOTENIN Ki = 16.0 nM 7.80
CHEMBL75029 Ki = 45.0 nM 7.35
CHEMBL39 SEROTONIN Ki = 78.0 nM 7.11
CHEMBL74378 Ki = 93.0 nM 7.03
CHEMBL306569 Ki = 183.0 nM 6.74