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Assay Detail

CHEMBL3744553

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

Binding
Displacement of [3H]mesulergine from 5HT2C receptor in rat brain cortex
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of amide, sulfonamide and urea benzisoxazole derivatives as potential atypical antipsychotics
Chen Y, Lan Y, Cao X, Xu X, Zhang J, Yu M, Liu X, Liu B, Zhang G
Medchemcomm (2015) 6 : 831 -838
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.81 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.48
CHEMBL85 RISPERIDONE 4.0 1 6.90
CHEMBL3740256 1 6.86
CHEMBL3741292 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 33.1 nM 7.48
CHEMBL85 RISPERIDONE Ki = 125.9 nM 6.90
CHEMBL3740256 Ki = 136.8 nM 6.86
CHEMBL3741292 Ki = 998.2 nM 6.00