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Assay Detail

CHEMBL645608

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

Functional
Alpha-2 adrenergic receptor antagonistic activity in human blood platelets.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Blood
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Zhang X, Yao XT, Dalton JT, Shams G, Lei L, Patil PN, Feller DR, Hsu FL, George C, Miller DD.
J Med Chem (1996) 39 : 3001 -3013
PubMed 8709134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.80 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77921 MEDETOMIDINE 3.0 1 5.54
CHEMBL105328 1 4.84
CHEMBL420652 1 4.01
CHEMBL322844 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77921 MEDETOMIDINE IC50 = 2900.0 nM 5.54
CHEMBL105328 IC50 = 14300.0 nM 4.84
CHEMBL420652 IC50 = 97700.0 nM 4.01
CHEMBL322844 IC50 = 215400.0 nM -