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Assay Detail

CHEMBL645479

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

Binding
Binding affinity towards human alpha-2 adrenergic receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
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 6.69 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.12
CHEMBL716 QUETIAPINE 4.0 1 7.06
CHEMBL42 CLOZAPINE 4.0 1 6.80
CHEMBL715 OLANZAPINE 4.0 1 6.64
CHEMBL708 ZIPRASIDONE 4.0 1 6.41
CHEMBL285802 ZOTEPINE 2.0 1 6.02
CHEMBL12713 SERTINDOLE 4.0 1 5.78
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 7.5 nM 8.12
CHEMBL716 QUETIAPINE Ki = 87.0 nM 7.06
CHEMBL42 CLOZAPINE Ki = 160.0 nM 6.80
CHEMBL715 OLANZAPINE Ki = 230.0 nM 6.64
CHEMBL708 ZIPRASIDONE Ki = 390.0 nM 6.41
CHEMBL285802 ZOTEPINE Ki = 960.0 nM 6.02
CHEMBL12713 SERTINDOLE Ki = 1680.0 nM 5.78
CHEMBL54 HALOPERIDOL Ki > 5000.0 nM -