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Assay Detail

CHEMBL617267

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

Binding
Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor rat frontal cortex membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
Fontenla JA, Osuna J, Rosa E, Castro ME, G-Ferreiro T, Loza-García I, Calleja JM, Sanz F, Rodríguez J, Raviña E.
J Med Chem (1994) 37 : 2564 -2573
PubMed 7914540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.26 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1065 METHYSERGIDE 4.0 1 8.84
CHEMBL87717 1 8.60
CHEMBL87458 1 8.42
CHEMBL87943 1 8.11
CHEMBL87026 1 7.89
CHEMBL54 HALOPERIDOL 4.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1065 METHYSERGIDE Ki = 1.445 nM 8.84
CHEMBL87717 Ki = 2.512 nM 8.60
CHEMBL87458 Ki = 3.802 nM 8.42
CHEMBL87943 Ki = 7.762 nM 8.11
CHEMBL87026 Ki = 12.88 nM 7.89
CHEMBL54 HALOPERIDOL Ki = 19.95 nM 7.70