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Assay Detail

CHEMBL643522

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

Binding
Binding affinity towards human alpha-1 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-1 (CHEMBL2094251)
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 7.95 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12713 SERTINDOLE 4.0 1 8.74
CHEMBL85 RISPERIDONE 4.0 1 8.64
CHEMBL285802 ZOTEPINE 2.0 1 8.47
CHEMBL708 ZIPRASIDONE 4.0 1 7.92
CHEMBL54 HALOPERIDOL 4.0 1 7.72
CHEMBL42 CLOZAPINE 4.0 1 7.64
CHEMBL716 QUETIAPINE 4.0 1 7.24
CHEMBL715 OLANZAPINE 4.0 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12713 SERTINDOLE Ki = 1.8 nM 8.74
CHEMBL85 RISPERIDONE Ki = 2.3 nM 8.64
CHEMBL285802 ZOTEPINE Ki = 3.4 nM 8.47
CHEMBL708 ZIPRASIDONE Ki = 12.0 nM 7.92
CHEMBL54 HALOPERIDOL Ki = 19.0 nM 7.72
CHEMBL42 CLOZAPINE Ki = 23.0 nM 7.64
CHEMBL716 QUETIAPINE Ki = 58.0 nM 7.24
CHEMBL715 OLANZAPINE Ki = 60.0 nM 7.22