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Assay Detail

CHEMBL643580

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

Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

A convenient synthesis of 2-amino-2-oxazolines and their pharmacological evaluation at cloned human adrenergic receptors
Wong WC, Wang D, Forray C, Vaysse PJ, Branchek TA, Gluchowski C
Bioorg Med Chem Lett (1994) 4 : 2317 -2322
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.74 8.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75030 1 8.93
CHEMBL310335 1 8.79
CHEMBL134 CLONIDINE 4.0 1 8.09
CHEMBL305928 1 7.42
CHEMBL306377 1 6.64
CHEMBL289480 RILMENIDINE 4.0 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75030 EC50 = 1.175 nM 8.93
CHEMBL310335 EC50 = 1.622 nM 8.79
CHEMBL134 CLONIDINE EC50 = 8.128 nM 8.09
CHEMBL305928 EC50 = 38.02 nM 7.42
CHEMBL306377 EC50 = 229.09 nM 6.64
CHEMBL289480 RILMENIDINE EC50 = 275.42 nM 6.56