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Assay Detail

CHEMBL616983

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

Binding
Inhibitory activity against 5-hydroxytryptamine 2 receptor by 3H ligand binding experiments.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds.
Kato S, Morie T, Kon T, Yoshida N, Karasawa T, Matsumoto J.
J Med Chem (1991) 34 : 616 -624
PubMed 1995885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.45 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1729 CISAPRIDE 4.0 1 8.01
CHEMBL86 METOCLOPRAMIDE 4.0 1 4.88
CHEMBL1733174 MOSAPRIDE CITRATE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1729 CISAPRIDE IC50 = 9.8 nM 8.01
CHEMBL86 METOCLOPRAMIDE IC50 = 13200.0 nM 4.88
CHEMBL1733174 MOSAPRIDE CITRATE IC50 > 100000.0 nM -