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Assay Detail

CHEMBL3058311

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

Binding
Competitive antagonist activity at alpha1D adrenergic receptor in Rattus norvegicus (rat) aorta assessed as inhibition of (-)-noradrenaline-induced contraction
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1D adrenergic receptor (CHEMBL326)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(+)-Cyclazosin Derivatives as 1-Adrenoceptor Antagonists
Sagratini G, Buccioni M, Gulini U, Marucci G, Melchiorre C, Leonardi A, Testa R, Giardina D
Med Chem Res (2004) 13 : 190 -199
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.05 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2261604 (+)-CYCLAZOSIN 1 7.27
CHEMBL2261605 1 7.23
CHEMBL2261607 1 7.05
CHEMBL2261606 1 7.04
CHEMBL2261608 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2261604 (+)-CYCLAZOSIN Kd = 53.7 nM 7.27
CHEMBL2261605 Kd = 58.88 nM 7.23
CHEMBL2261607 Kd = 89.13 nM 7.05
CHEMBL2261606 Kd = 91.2 nM 7.04
CHEMBL2261608 Kd = 213.8 nM 6.67