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Assay Detail

CHEMBL772607

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

Functional
In vitro antagonist activity against (-)-phenylephrine or (-)-norepinephrine-induced alpha1-adrenoceptor-mediated vasoconstriction of rabbit isolated pulmonary artery.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
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 3 6.80 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1732 DIHYDROERGOTAMINE 4.0 1 7.55
CHEMBL2110596 AZAPETINE -1.0 1 6.96
CHEMBL10347 RAUWOLSCINE 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1732 DIHYDROERGOTAMINE Kd = 28.18 nM 7.55
CHEMBL2110596 AZAPETINE Kd = 109.65 nM 6.96
CHEMBL10347 RAUWOLSCINE Kd = 1288.25 nM 5.89