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Assay Detail

CHEMBL803828

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

Binding
Tested for the binding affinity towards 5-HT2 receptor measured by [3H]ketanserin binding to frontal cerebral cortex membranes of rat
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

5-HT2 antagonist activity of 3-aminomethyltetralones
Loza M, Verde I, Castro M, Orallo F, Fontenla J, Calleja J, Ravina E, Cortizo L, de Ceballos M
Bioorg Med Chem Lett (1991) 1 : 717 -720
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.73 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1065 METHYSERGIDE 4.0 1 8.84
CHEMBL308480 1 8.80
CHEMBL72649 1 7.29
CHEMBL310734 1 7.25
CHEMBL310153 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1065 METHYSERGIDE Ki = 1.445 nM 8.84
CHEMBL308480 Ki = 1.585 nM 8.80
CHEMBL72649 Ki = 51.29 nM 7.29
CHEMBL310734 Ki = 56.23 nM 7.25
CHEMBL310153 Ki = 331.13 nM 6.48