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Assay Detail

CHEMBL770729

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

Functional
Inhibition of phenylephrine-induced contraction of the rabbit aorta as a measure of functional alpha-1-adrenoceptor antagonism
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist.
Clark RD, Repke DB, Kilpatrick AT, Brown CM, MacKinnon AC, Clague RU, Spedding M.
J Med Chem (1989) 32 : 2034 -2036
PubMed 2570150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 5.55 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279807 1 6.10
CHEMBL62833 1 5.00
CHEMBL62912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279807 Kd = 794.33 nM 6.10
CHEMBL62833 Kd = 10000.0 nM 5.00
CHEMBL62912 Kd > 1000.0 nM -