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Assay Detail

CHEMBL618163

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

Binding
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives.
López-Rodríguez ML, Porras E, Morcillo MJ, Benhamú B, Soto LJ, Lavandera JL, Ramos JA, Olivella M, Campillo M, Pardo L.
J Med Chem (2003) 46 : 5638 -5650
PubMed 14667218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.74 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69257 1 8.70
CHEMBL428494 1 8.70
CHEMBL12427 1 8.50
CHEMBL273246 1 8.40
CHEMBL13052 1 8.30
CHEMBL12702 1 8.30
CHEMBL268921 1 7.00
CHEMBL273890 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69257 Ki = 1.995 nM 8.70
CHEMBL428494 Ki = 1.995 nM 8.70
CHEMBL12427 Ki = 3.162 nM 8.50
CHEMBL273246 Ki = 3.981 nM 8.40
CHEMBL13052 Ki = 5.012 nM 8.30
CHEMBL12702 Ki = 5.012 nM 8.30
CHEMBL268921 Ki = 100.0 nM 7.00
CHEMBL273890 Ki = 100000.0 nM 4.00