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Assay Detail

CHEMBL687415

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

Functional
Ability to reverse inhibitory effects of UK-14304 on the contraction of guinea pig ileum as a measure of alpha-2 adrenergic receptor antagonism.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

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 4 8.58 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279807 1 9.70
CHEMBL62912 1 9.70
CHEMBL10316 IDAZOXAN 3.0 1 8.40
CHEMBL62833 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279807 Kd = 0.1995 nM 9.70
CHEMBL62912 Kd = 0.1995 nM 9.70
CHEMBL10316 IDAZOXAN Kd = 3.981 nM 8.40
CHEMBL62833 Kd = 316.23 nM 6.50