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Assay Detail

CHEMBL617275

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

Binding
Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective optimization of side activities: another way for drug discovery.
Wermuth CG.
J Med Chem (2004) 47 : 1303 -1314
PubMed 14998318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.71 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12713 SERTINDOLE 4.0 1 8.89
CHEMBL285802 ZOTEPINE 2.0 1 8.54
CHEMBL715 OLANZAPINE 4.0 1 8.15
CHEMBL708 ZIPRASIDONE 4.0 1 7.89
CHEMBL42 CLOZAPINE 4.0 1 7.89
CHEMBL85 RISPERIDONE 4.0 1 7.20
CHEMBL716 QUETIAPINE 4.0 1 5.42
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12713 SERTINDOLE Ki = 1.3 nM 8.89
CHEMBL285802 ZOTEPINE Ki = 2.9 nM 8.54
CHEMBL715 OLANZAPINE Ki = 7.1 nM 8.15
CHEMBL708 ZIPRASIDONE Ki = 13.0 nM 7.89
CHEMBL42 CLOZAPINE Ki = 13.0 nM 7.89
CHEMBL85 RISPERIDONE Ki = 63.0 nM 7.20
CHEMBL716 QUETIAPINE Ki = 3820.0 nM 5.42
CHEMBL54 HALOPERIDOL Ki > 5000.0 nM -