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Assay Detail

CHEMBL984240

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Functional
Agonist activity at alpha2 adrenoceptor in human cortical membrane after 2 hrs by [35S]GTPgammaS binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor ligands: searching for structure-activity relationships.
Rodriguez F, Rozas I, Ortega JE, Erdozain AM, Meana JJ, Callado LF, Callado LF.
J Med Chem (2009) 52 : 601 -609
PubMed 19133776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 4.63 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473567 1 5.72
CHEMBL844 BRIMONIDINE 4.0 1 4.94
CHEMBL482359 1 4.79
CHEMBL482200 1 4.41
CHEMBL506313 1 4.23
CHEMBL467525 1 4.21
CHEMBL509581 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473567 EC50 = 1900.0 nM 5.72
CHEMBL844 BRIMONIDINE EC50 = 11400.0 nM 4.94
CHEMBL482359 EC50 = 16200.0 nM 4.79
CHEMBL482200 EC50 = 38700.0 nM 4.41
CHEMBL506313 EC50 = 59300.0 nM 4.23
CHEMBL467525 EC50 = 61400.0 nM 4.21
CHEMBL509581 EC50 = 82300.0 nM 4.08