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Assay Detail

CHEMBL3875675

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

ADMET
Displacement of [3H]mesulergine from 5-HT2C receptor in Sprague-Dawley rat cerebral cortex incubated for 15 mins in presence of spiperone by liquid scintillation counting analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
Cao X, Chen Y, Zhang Y, Qiu Y, Yu M, Xu X, Liu X, Liu BF, Zhang G.
Eur J Med Chem (2016) 124 : 713 -728
PubMed 27639363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.43 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3884161 1 9.00
CHEMBL3884325 1 8.04
CHEMBL85 RISPERIDONE 4.0 1 7.57
CHEMBL3885471 1 6.75
CHEMBL3883955 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3884161 Ki = 1.0 nM 9.00
CHEMBL3884325 Ki = 9.1 nM 8.04
CHEMBL85 RISPERIDONE Ki = 26.7 nM 7.57
CHEMBL3885471 Ki = 177.0 nM 6.75
CHEMBL3883955 Ki = 1584.0 nM 5.80