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Assay Detail

CHEMBL1104417

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

Binding
Displacement of [3H]5CT from 5HT7 receptor
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 Autocuration

Target

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

Publication

The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists.
Kurczab R, Nowak M, Chilmonczyk Z, Sylte I, Bojarski AJ.
Bioorg Med Chem Lett (2010) 20 : 2465 -2468
PubMed 20346662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.17 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363452 1 9.70
CHEMBL430706 1 9.17
CHEMBL281923 1 8.96
CHEMBL25815 1 8.67
CHEMBL19215 METERGOLINE 2.0 1 8.20
CHEMBL42 CLOZAPINE 4.0 1 7.40
CHEMBL1091933 1 6.71
CHEMBL1094908 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363452 Ki = 0.1995 nM 9.70
CHEMBL430706 Ki = 0.6761 nM 9.17
CHEMBL281923 Ki = 1.096 nM 8.96
CHEMBL25815 Ki = 2.138 nM 8.67
CHEMBL19215 METERGOLINE Ki = 6.31 nM 8.20
CHEMBL42 CLOZAPINE Ki = 39.81 nM 7.40
CHEMBL1091933 Ki = 197.0 nM 6.71
CHEMBL1094908 Ki = 265.0 nM 6.58