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Assay Detail

CHEMBL977364

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

Binding
Inhibition of voltage-dependent N-type calcium channel in human IMR32 cells assessed as effect on calcium influx
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels.
Yamamoto T, Niwa S, Ohno S, Tokumasu M, Masuzawa Y, Nakanishi C, Nakajo A, Onishi T, Koganei H, Fujita S, Takeda T, Kito M, Ono Y, Saitou Y, Takahara A, Iwata S, Shoji M.
Bioorg Med Chem Lett (2008) 18 : 4813 -4816
PubMed 18684623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.68 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL453084 1 6.09
CHEMBL382072 1 6.00
CHEMBL453088 1 5.85
CHEMBL452076 CILNIDIPINE 3.0 1 5.80
CHEMBL453604 1 5.77
CHEMBL370409 1 5.77
CHEMBL453605 1 5.75
CHEMBL511062 1 5.75
CHEMBL452072 1 5.70
CHEMBL451817 1 5.68
CHEMBL508180 1 5.60
CHEMBL452073 1 5.52
CHEMBL451812 1 5.52
CHEMBL508181 1 5.46
CHEMBL451813 1 5.41
CHEMBL451811 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL453084 IC50 = 810.0 nM 6.09
CHEMBL382072 IC50 = 1000.0 nM 6.00
CHEMBL453088 IC50 = 1400.0 nM 5.85
CHEMBL452076 CILNIDIPINE IC50 = 1600.0 nM 5.80
CHEMBL453604 IC50 = 1700.0 nM 5.77
CHEMBL370409 IC50 = 1700.0 nM 5.77
CHEMBL453605 IC50 = 1800.0 nM 5.75
CHEMBL511062 IC50 = 1800.0 nM 5.75
CHEMBL452072 IC50 = 2000.0 nM 5.70
CHEMBL451817 IC50 = 2100.0 nM 5.68
CHEMBL508180 IC50 = 2500.0 nM 5.60
CHEMBL452073 IC50 = 3000.0 nM 5.52
CHEMBL451812 IC50 = 3000.0 nM 5.52
CHEMBL508181 IC50 = 3500.0 nM 5.46
CHEMBL451813 IC50 = 3900.0 nM 5.41
CHEMBL451811 IC50 = 5800.0 nM 5.24