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Assay Detail

CHEMBL770732

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

Binding
Inhibition of specific [3H]-prazosin binding (0.2 nM) to rat brain membranes alpha1 adrenoceptor.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
Timmermans PB, de Jonge A, Thoolen MJ, Wilffert B, Batink H, van Zwieten PA.
J Med Chem (1984) 27 : 495 -503
PubMed 6142954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.55 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597 PHENTOLAMINE 4.0 1 7.41
CHEMBL42 CLOZAPINE 4.0 1 6.90
CHEMBL6437 MIANSERIN 4.0 1 6.42
CHEMBL31836 PIPEROXAN 2.0 1 6.14
CHEMBL15245 YOHIMBINE 3.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597 PHENTOLAMINE IC50 = 39.0 nM 7.41
CHEMBL42 CLOZAPINE IC50 = 125.0 nM 6.90
CHEMBL6437 MIANSERIN IC50 = 380.0 nM 6.42
CHEMBL31836 PIPEROXAN IC50 = 720.0 nM 6.14
CHEMBL15245 YOHIMBINE IC50 = 1300.0 nM 5.89