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Assay Detail

CHEMBL782875

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

Functional
Calcium antagonistic activity was evaluated by in vitro inhibition of [3H]nitrendipine binding on rat cerebral cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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 8.76 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1484 NICARDIPINE 4.0 1 10.59
CHEMBL540511 1 10.22
CHEMBL2093965 1 9.00
CHEMBL542814 1 8.47
CHEMBL2 PRAZOSIN 4.0 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1484 NICARDIPINE IC50 = 0.026 nM 10.59
CHEMBL540511 IC50 = 0.06 nM 10.22
CHEMBL2093965 IC50 = 1.0 nM 9.00
CHEMBL542814 IC50 = 3.4 nM 8.47
CHEMBL2 PRAZOSIN IC50 = 3000.0 nM 5.52