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Assay Detail

CHEMBL1016579

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

Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 18 6.69 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10332 1 9.10
CHEMBL10316 IDAZOXAN 3.0 1 7.75
CHEMBL495096 1 7.57
CHEMBL494885 1 7.19
CHEMBL451229 1 7.11
CHEMBL495095 ALLYPHENYLINE 1 7.07
CHEMBL128168 BIPHENYLINE 1 6.70
CHEMBL523048 1 6.69
CHEMBL492648 1 6.61
CHEMBL273485 1 6.58
CHEMBL492639 1 6.47
CHEMBL495097 1 6.17
CHEMBL522151 1 6.16
CHEMBL493272 1 6.08
CHEMBL493675 1 6.04
CHEMBL492445 1 5.90
CHEMBL492444 1 5.80
CHEMBL442815 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10332 Ki = 0.7943 nM 9.10
CHEMBL10316 IDAZOXAN Ki = 17.78 nM 7.75
CHEMBL495096 Ki = 26.92 nM 7.57
CHEMBL494885 Ki = 64.57 nM 7.19
CHEMBL451229 Ki = 77.62 nM 7.11
CHEMBL495095 ALLYPHENYLINE Ki = 85.11 nM 7.07
CHEMBL128168 BIPHENYLINE Ki = 199.53 nM 6.70
CHEMBL523048 Ki = 204.17 nM 6.69
CHEMBL492648 Ki = 245.47 nM 6.61
CHEMBL273485 Ki = 263.03 nM 6.58
CHEMBL492639 Ki = 338.84 nM 6.47
CHEMBL495097 Ki = 676.08 nM 6.17
CHEMBL522151 Ki = 691.83 nM 6.16
CHEMBL493272 Ki = 831.76 nM 6.08
CHEMBL493675 Ki = 912.01 nM 6.04
CHEMBL492445 Ki = 1258.93 nM 5.90
CHEMBL492444 Ki = 1584.89 nM 5.80
CHEMBL442815 Ki = 3090.3 nM 5.51