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Assay Detail

CHEMBL2390229

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

Binding
Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
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 investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
Chen Y, Wang S, Xu X, Liu X, Yu M, Zhao S, Liu S, Qiu Y, Zhang T, Liu BF, Zhang G.
J Med Chem (2013) 56 : 4671 -4690
PubMed 23675993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.94 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2387260 1 7.92
CHEMBL85 RISPERIDONE 4.0 1 7.84
CHEMBL42 CLOZAPINE 4.0 1 7.79
CHEMBL2387230 1 7.16
CHEMBL2387265 1 6.59
CHEMBL2385102 1 6.41
CHEMBL2387253 1 6.00
CHEMBL2387229 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2387260 Ki = 11.9 nM 7.92
CHEMBL85 RISPERIDONE Ki = 14.5 nM 7.84
CHEMBL42 CLOZAPINE Ki = 16.2 nM 7.79
CHEMBL2387230 Ki = 68.9 nM 7.16
CHEMBL2387265 Ki = 256.2 nM 6.59
CHEMBL2385102 Ki = 389.3 nM 6.41
CHEMBL2387253 Ki = 999.5 nM 6.00
CHEMBL2387229 Ki = 1700.7 nM 5.77