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Assay Detail

CHEMBL641384

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

Binding
Tested for its inhibitory activity against alpha-2 adrenoceptor in guinea pig ileum
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
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
EC50 7 7.20 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77921 MEDETOMIDINE 3.0 1 8.52
CHEMBL306751 3 8.05
CHEMBL544765 1 7.75
CHEMBL542155 1 6.43
CHEMBL553835 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77921 MEDETOMIDINE EC50 = 3.0 nM 8.52
CHEMBL306751 EC50 = 9.0 nM 8.05
CHEMBL306751 EC50 = 11.0 nM 7.96
CHEMBL544765 EC50 = 18.0 nM 7.75
CHEMBL542155 EC50 = 375.0 nM 6.43
CHEMBL553835 EC50 = 32992.0 nM 4.48
CHEMBL306751 EC50 = - nM -