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Assay Detail

CHEMBL864733

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

Functional
Inhibitory activity against N-type calcium channel by calcium influx into IMR32 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Expert

Publication

Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels.
Yamamoto T, Niwa S, Ohno S, Onishi T, Matsueda H, Koganei H, Uneyama H, Fujita S, Takeda T, Kito M, Ono Y, Saitou Y, Takahara A, Iwata S, Shoji M.
Bioorg Med Chem Lett (2006) 16 : 798 -802
PubMed 16309909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.48 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201566 1 6.17
CHEMBL369934 1 6.10
CHEMBL201984 1 6.08
CHEMBL203041 1 6.05
CHEMBL201860 1 6.00
CHEMBL382072 1 6.00
CHEMBL201258 1 5.96
CHEMBL201306 1 5.89
CHEMBL382528 1 5.82
CHEMBL452076 CILNIDIPINE 3.0 1 5.80
CHEMBL370409 1 5.77
CHEMBL201057 1 5.77
CHEMBL202374 1 5.75
CHEMBL202464 1 5.70
CHEMBL382236 1 5.54
CHEMBL508181 1 5.46
CHEMBL372748 1 5.41
CHEMBL201599 1 5.35
CHEMBL201257 1 5.34
CHEMBL202459 1 5.21
CHEMBL380499 1 5.00
CHEMBL382629 1 4.96
CHEMBL382450 1 4.68
CHEMBL203470 1 4.62
CHEMBL202605 1 4.55
CHEMBL201401 1 4.43
CHEMBL204486 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201566 IC50 = 680.0 nM 6.17
CHEMBL369934 IC50 = 790.0 nM 6.10
CHEMBL201984 IC50 = 830.0 nM 6.08
CHEMBL203041 IC50 = 890.0 nM 6.05
CHEMBL201860 IC50 = 1000.0 nM 6.00
CHEMBL382072 IC50 = 1000.0 nM 6.00
CHEMBL201258 IC50 = 1100.0 nM 5.96
CHEMBL201306 IC50 = 1300.0 nM 5.89
CHEMBL382528 IC50 = 1500.0 nM 5.82
CHEMBL452076 CILNIDIPINE IC50 = 1600.0 nM 5.80
CHEMBL370409 IC50 = 1700.0 nM 5.77
CHEMBL201057 IC50 = 1700.0 nM 5.77
CHEMBL202374 IC50 = 1800.0 nM 5.75
CHEMBL202464 IC50 = 2000.0 nM 5.70
CHEMBL382236 IC50 = 2900.0 nM 5.54
CHEMBL508181 IC50 = 3500.0 nM 5.46
CHEMBL372748 IC50 = 3900.0 nM 5.41
CHEMBL201599 IC50 = 4500.0 nM 5.35
CHEMBL201257 IC50 = 4600.0 nM 5.34
CHEMBL202459 IC50 = 6200.0 nM 5.21
CHEMBL380499 IC50 = 10000.0 nM 5.00
CHEMBL382629 IC50 = 11000.0 nM 4.96
CHEMBL382450 IC50 = 21000.0 nM 4.68
CHEMBL203470 IC50 = 24000.0 nM 4.62
CHEMBL202605 IC50 = 28000.0 nM 4.55
CHEMBL201401 IC50 = 37000.0 nM 4.43
CHEMBL204486 IC50 = 37000.0 nM 4.43