Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL648824

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

Binding
Compound was measured in vivo for its binding affinity at Alpha-1 adrenergic receptor using [3H]prazosin as radioligand.
6
Total Activities
6
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

Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptor
Baxter EW, Reitz AB
Bioorg Med Chem Lett (1997) 7 : 763 -768
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.07 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10085 MAZAPERTINE 2.0 1 8.89
CHEMBL61440 1 8.77
CHEMBL165364 1 8.54
CHEMBL423632 1 7.44
CHEMBL164330 1 6.70
CHEMBL423642 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10085 MAZAPERTINE Ki = 1.3 nM 8.89
CHEMBL61440 Ki = 1.7 nM 8.77
CHEMBL165364 Ki = 2.9 nM 8.54
CHEMBL423632 Ki = 36.0 nM 7.44
CHEMBL164330 Ki = 200.0 nM 6.70
CHEMBL423642 Ki > 1000.0 nM -