Assay Detail

CHEMBL647411

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Functional

Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-2 adrenergic receptor

ChEMBL ↗

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Target

Adrenergic receptor alpha-2 (CHEMBL2095158) ↗

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Primary target Adrenergic receptor alpha-2

CHEMBL2095158

Anchored from Assay target.

Protein identity Adrenergic receptor alpha-2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Oryctolagus cuniculus
Confidence	4 — Cell-line / Tissue
Curated By	Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158) ↗

Type	PROTEIN FAMILY
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
EC50	2	8.54	8.72

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL647	APRACLONIDINE	4.0	1	8.72
CHEMBL134	CLONIDINE	4.0	1	8.36

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL647	APRACLONIDINE	EC50	=	1.9	nM	8.72
CHEMBL134	CLONIDINE	EC50	=	4.4	nM	8.36