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Assay Detail

CHEMBL643907

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

Binding
In vitro inhibitory activity was evaluated against,[3H]clonidine (Clon) rat brain minus cerebellum Alpha-2 adrenergic receptor
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
Nordmann R, Widmer A.
J Med Chem (1985) 28 : 1540 -1542
PubMed 4045929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.77 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 6.37
CHEMBL38992 ETISULERGINE 2.0 1 6.32
CHEMBL2218861 QUINAGOLIDE 4.0 3 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE IC50 = 430.0 nM 6.37
CHEMBL38992 ETISULERGINE IC50 = 480.0 nM 6.32
CHEMBL2218861 QUINAGOLIDE IC50 = 5600.0 nM 5.25
CHEMBL2218861 QUINAGOLIDE IC50 = 7400.0 nM 5.13
CHEMBL2218861 QUINAGOLIDE IC50 > 10000.0 nM -