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Assay Detail

CHEMBL616893

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

Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2A receptor in HEK293 cells, using [3H]ketanserin as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Bromidge SM, Clarke SE, King FD, Lovell PJ, Newman H, Riley G, Routledge C, Serafinowska HT, Smith DR, Thomas DR.
Bioorg Med Chem Lett (2002) 12 : 1357 -1360
PubMed 11992776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.18 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29433 1 6.60
CHEMBL29410 1 6.20
CHEMBL29846 1 6.00
CHEMBL282971 1 5.90
CHEMBL431298 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29433 Ki = 251.19 nM 6.60
CHEMBL29410 Ki = 630.96 nM 6.20
CHEMBL29846 Ki = 1000.0 nM 6.00
CHEMBL282971 Ki = 1258.93 nM 5.90
CHEMBL431298 Ki < 2511.89 nM -