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Assay Detail

CHEMBL649804

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

Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
Hong SS, Romstedt KJ, Feller DR, Hsu FL, Cupps TL, Lyon RA, Miller DD.
J Med Chem (1994) 37 : 2328 -2333
PubMed 7914537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.17 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306751 3 5.89
CHEMBL544765 1 5.52
CHEMBL77921 MEDETOMIDINE 3.0 1 5.47
CHEMBL542155 1 4.21
CHEMBL553835 1 -
CHEMBL75022 1 -
CHEMBL541302 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306751 IC50 = 1300.0 nM 5.89
CHEMBL544765 IC50 = 3000.0 nM 5.52
CHEMBL77921 MEDETOMIDINE IC50 = 3400.0 nM 5.47
CHEMBL306751 IC50 = 9100.0 nM 5.04
CHEMBL306751 IC50 = 12300.0 nM 4.91
CHEMBL542155 IC50 = 61900.0 nM 4.21
CHEMBL553835 IC50 = 379800.0 nM -
CHEMBL75022 IC50 = 580400.0 nM -
CHEMBL541302 IC50 > 300000.0 nM -