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Assay Detail

CHEMBL647722

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

Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
Munk SA, Harcourt D, Ambrus G, Denys L, Gluchowski C, Burke JA, Kharlamb AB, Manlapaz CA, Padillo EU, Runde E, Williams L, Wheeler LA, Garst ME.
J Med Chem (1996) 39 : 3533 -3538
PubMed 8784451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.52 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298936 1 8.92
CHEMBL49137 1 8.70
CHEMBL647 APRACLONIDINE 4.0 1 8.54
CHEMBL134 CLONIDINE 4.0 1 8.42
CHEMBL49284 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298936 Ki = 1.2 nM 8.92
CHEMBL49137 Ki = 2.0 nM 8.70
CHEMBL647 APRACLONIDINE Ki = 2.9 nM 8.54
CHEMBL134 CLONIDINE Ki = 3.8 nM 8.42
CHEMBL49284 Ki = 9.6 nM 8.02