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Assay Detail

CHEMBL620785

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

Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Bromidge SM, Brown AM, Clarke SE, Dodgson K, Gager T, Grassam HL, Jeffrey PM, Joiner GF, King FD, Middlemiss DN, Moss SF, Newman H, Riley G, Routledge C, Wyman P.
J Med Chem (1999) 42 : 202 -205
PubMed 9925723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.24 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29846 1 9.20
CHEMBL62368 1 9.10
CHEMBL62538 1 9.10
CHEMBL291618 1 9.00
CHEMBL61318 1 8.90
CHEMBL542139 1 8.90
CHEMBL304039 1 8.70
CHEMBL60264 1 8.60
CHEMBL409160 1 8.50
CHEMBL292759 1 8.30
CHEMBL60669 1 8.00
CHEMBL46071 1 7.90
CHEMBL433461 1 7.30
CHEMBL62594 1 7.20
CHEMBL302845 1 7.10
CHEMBL64715 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29846 Ki = 0.631 nM 9.20
CHEMBL62368 Ki = 0.7943 nM 9.10
CHEMBL62538 Ki = 0.7943 nM 9.10
CHEMBL291618 Ki = 1.0 nM 9.00
CHEMBL61318 Ki = 1.259 nM 8.90
CHEMBL542139 Ki = 1.259 nM 8.90
CHEMBL304039 Ki = 1.995 nM 8.70
CHEMBL60264 Ki = 2.512 nM 8.60
CHEMBL409160 Ki = 3.162 nM 8.50
CHEMBL292759 Ki = 5.012 nM 8.30
CHEMBL60669 Ki = 10.0 nM 8.00
CHEMBL46071 Ki = 12.59 nM 7.90
CHEMBL433461 Ki = 50.12 nM 7.30
CHEMBL62594 Ki = 63.1 nM 7.20
CHEMBL302845 Ki = 79.43 nM 7.10
CHEMBL64715 Ki = 794.33 nM 6.10