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Assay Detail

CHEMBL642292

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

Binding
Binding affinity against alpha-2 adrenergic receptor in rat cerebral cortical membrane, determined using [3H]- yohimbine as the radioligand.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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
Ki 4 8.23 9.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279807 1 9.45
CHEMBL62912 1 9.18
CHEMBL10316 IDAZOXAN 3.0 1 7.96
CHEMBL62833 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279807 Ki = 0.3548 nM 9.45
CHEMBL62912 Ki = 0.6607 nM 9.18
CHEMBL10316 IDAZOXAN Ki = 10.96 nM 7.96
CHEMBL62833 Ki = 478.63 nM 6.32