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Assay Detail

CHEMBL1780797

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Binding
Inhibition of Voltage-dependent L-type calcium channel in rat thoracic aorta ring
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Thoracic aorta
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Voltage-gated L-type calcium channel (CHEMBL2095177)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Asymmetric synthesis and biological evaluations of (+)- and (-)-6-dimethoxymethyl-1,4-dihydropyridine-3-carboxylic acid derivatives blocking N-type calcium channels.
Yamamoto T, Ohno S, Niwa S, Tokumasu M, Hagihara M, Koganei H, Fujita S, Takeda T, Saitou Y, Iwayama S, Takahara A, Iwata S, Shoji M.
Bioorg Med Chem Lett (2011) 21 : 3317 -3319
PubMed 21514827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.40 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452076 CILNIDIPINE 3.0 1 8.96
CHEMBL508181 1 7.34
CHEMBL451812 3 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452076 CILNIDIPINE IC50 = 1.1 nM 8.96
CHEMBL508181 IC50 = 46.0 nM 7.34
CHEMBL451812 IC50 = 1800.0 nM 5.75
CHEMBL451812 IC50 = 8100.0 nM 5.09
CHEMBL451812 IC50 = 13200.0 nM 4.88