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Assay Detail

CHEMBL647810

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 alpha-1 adrenergic receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Kd 4 6.98 7.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597 PHENTOLAMINE 4.0 1 7.49
CHEMBL42 CLOZAPINE 4.0 1 7.43
CHEMBL31410 CORYNANTHEINE 1 6.60
CHEMBL15245 YOHIMBINE 3.0 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597 PHENTOLAMINE Kd = 32.36 nM 7.49
CHEMBL42 CLOZAPINE Kd = 37.15 nM 7.43
CHEMBL31410 CORYNANTHEINE Kd = 251.19 nM 6.60
CHEMBL15245 YOHIMBINE Kd = 398.11 nM 6.40