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Assay Detail

CHEMBL875101

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

Binding
Ability to displace the radioligand [3H]5-carboximidotryptamine ([3H]-5-CT) from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS-7
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.
Kikuchi C, Suzuki H, Hiranuma T, Koyama M.
Bioorg Med Chem Lett (2003) 13 : 61 -64
PubMed 12467617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.45 8.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL422869 1 8.69
CHEMBL69257 1 8.67
CHEMBL418888 1 8.45
CHEMBL348410 1 8.30
CHEMBL348890 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL422869 Ki = 2.042 nM 8.69
CHEMBL69257 Ki = 2.138 nM 8.67
CHEMBL418888 Ki = 3.548 nM 8.45
CHEMBL348410 Ki = 5.012 nM 8.30
CHEMBL348890 Ki = 7.244 nM 8.14