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

CHEMBL646301

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

Functional
Alpha-1 adrenergic receptor antagonist activity against agonist (norepinephrine) in isolated rat vas deferens
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

2-[[[2-(2,6-Dimethoxyphenoxy)ethyl]amino]-methyl] -1,4-benzoxathian: a new antagonist with high potency and selectivity toward alpha 1-adrenoreceptors.
Melchiorre C, Brasili L, Giardinà D, Pigini M, Strappaghetti G.
J Med Chem (1984) 27 : 1535 -1536
PubMed 6150111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 8.94 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL544713 BENOXATHIAN HYDROCHLORIDE 1 9.26
CHEMBL556001 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) 1 8.83
CHEMBL2 PRAZOSIN 4.0 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL544713 BENOXATHIAN HYDROCHLORIDE Kd = 0.5495 nM 9.26
CHEMBL556001 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) Kd = 1.479 nM 8.83
CHEMBL2 PRAZOSIN Kd = 1.82 nM 8.74