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Assay Detail

CHEMBL616229

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor (human cloned receptor) in HEK293 cells using [3H]8-OH-DPAT 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 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Lovell PJ, Bromidge SM, Dabbs S, Duckworth DM, Forbes IT, Jennings AJ, King FD, Middlemiss DN, Rahman SK, Saunders DV, Collin LL, Hagan JJ, Riley GJ, Thomas DR.
J Med Chem (2000) 43 : 342 -345
PubMed 10669560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.18 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333784 1 6.50
CHEMBL116448 1 6.40
CHEMBL94984 1 6.00
CHEMBL1788231 1 5.80
CHEMBL282199 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333784 Ki = 316.23 nM 6.50
CHEMBL116448 Ki = 398.11 nM 6.40
CHEMBL94984 Ki = 1000.0 nM 6.00
CHEMBL1788231 Ki = 1584.89 nM 5.80
CHEMBL282199 Ki < 10000.0 nM -