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Assay Detail

CHEMBL1016581

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

Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
17
Total Activities
17
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 Autocuration

Target

Alpha-2C adrenergic receptor (CHEMBL1916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
Gentili F, Cardinaletti C, Vesprini C, Carrieri A, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Laurila JM, Huhtinen A, Scheinin M, Pigini M.
J Med Chem (2008) 51 : 4289 -4299
PubMed 18578476 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.56 8.00
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495096 1 8.00
CHEMBL451229 1 7.68
CHEMBL495095 ALLYPHENYLINE 1 7.30
CHEMBL128168 BIPHENYLINE 1 7.24
CHEMBL493675 1 6.90
CHEMBL442815 1 6.30
CHEMBL523048 1 6.11
CHEMBL493272 1 6.10
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.10
CHEMBL492639 1 6.00
CHEMBL522151 1 5.50
CHEMBL495097 1 5.45
CHEMBL493674 1 -
CHEMBL492648 1 -
CHEMBL492647 1 -
CHEMBL492445 1 -
CHEMBL492444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495096 EC50 = 10.0 nM 8.00
CHEMBL451229 EC50 = 20.89 nM 7.68
CHEMBL495095 ALLYPHENYLINE EC50 = 50.12 nM 7.30
CHEMBL128168 BIPHENYLINE EC50 = 57.54 nM 7.24
CHEMBL493675 EC50 = 125.89 nM 6.90
CHEMBL442815 EC50 = 501.19 nM 6.30
CHEMBL523048 EC50 = 776.25 nM 6.11
CHEMBL493272 EC50 = 794.33 nM 6.10
CHEMBL1437 NOREPINEPHRINE EC50 = 794.33 nM 6.10
CHEMBL492639 EC50 = 1000.0 nM 6.00
CHEMBL522151 EC50 = 3162.28 nM 5.50
CHEMBL495097 EC50 = 3548.13 nM 5.45
CHEMBL493674 Activity - -
CHEMBL492648 Activity - -
CHEMBL492647 Activity - -
CHEMBL492445 Activity - -
CHEMBL492444 Activity - -