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Assay Detail

CHEMBL918090

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

Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.
Gentili F, Ghelfi F, Giannella M, Piergentili A, Pigini M, Quaglia W, Vesprini C, Crassous PA, Paris H, Carrieri A.
J Med Chem (2004) 47 : 6160 -6173
PubMed 15566287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 16 - -
EC50 9 6.65 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223829 1 7.38
CHEMBL385310 1 7.12
CHEMBL223836 1 6.98
CHEMBL128168 BIPHENYLINE 1 6.94
CHEMBL222371 1 6.59
CHEMBL373535 1 6.50
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.43
CHEMBL130884 1 6.41
CHEMBL222933 1 5.46
CHEMBL221989 1 -
CHEMBL222593 1 -
CHEMBL222592 1 -
CHEMBL222591 1 -
CHEMBL1204386 1 -
CHEMBL374954 1 -
CHEMBL221523 1 -
CHEMBL222928 1 -
CHEMBL222138 1 -
CHEMBL222798 1 -
CHEMBL374584 1 -
CHEMBL426900 1 -
CHEMBL222973 1 -
CHEMBL223830 1 -
CHEMBL442045 1 -
CHEMBL373830 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223829 EC50 = 41.69 nM 7.38
CHEMBL385310 EC50 = 75.86 nM 7.12
CHEMBL223836 EC50 = 104.71 nM 6.98
CHEMBL128168 BIPHENYLINE EC50 = 114.82 nM 6.94
CHEMBL222371 EC50 = 257.04 nM 6.59
CHEMBL373535 EC50 = 316.23 nM 6.50
CHEMBL1437 NOREPINEPHRINE EC50 = 371.54 nM 6.43
CHEMBL130884 EC50 = 389.05 nM 6.41
CHEMBL222933 EC50 = 3467.37 nM 5.46
CHEMBL221989 Activity - -
CHEMBL222593 Activity - -
CHEMBL222592 Activity - -
CHEMBL222591 Activity - -
CHEMBL1204386 Activity - -
CHEMBL374954 Activity - -
CHEMBL221523 Activity - -
CHEMBL222928 Activity - -
CHEMBL222138 Activity - -
CHEMBL222798 Activity - -
CHEMBL374584 Activity - -
CHEMBL426900 Activity - -
CHEMBL222973 Activity - -
CHEMBL223830 Activity - -
CHEMBL442045 Activity - -
CHEMBL373830 Activity - -