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Assay Detail

CHEMBL645515

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

Binding
Alpha-2-adrenolytic activity was assessed from the ability to inhibit [3H]yohimbine binding to rat cerebral cortex preparation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
Marciniak G, Delgado A, Leclerc G, Velly J, Decker N, Schwartz J.
J Med Chem (1989) 32 : 1402 -1407
PubMed 2542561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.81 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3350238 1 6.68
CHEMBL540511 1 6.08
CHEMBL1484 NICARDIPINE 4.0 1 5.85
CHEMBL542814 1 5.70
CHEMBL2093965 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3350238 IC50 = 210.0 nM 6.68
CHEMBL540511 IC50 = 830.0 nM 6.08
CHEMBL1484 NICARDIPINE IC50 = 1400.0 nM 5.85
CHEMBL542814 IC50 = 2000.0 nM 5.70
CHEMBL2093965 IC50 = 19000.0 nM 4.72