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Assay Detail

CHEMBL653726

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

Binding
Inhibition of [3H]nitrendipine binding to guinea pig ileal longitudinal smooth muscle
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Muscle tissue
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Voltage-gated L-type calcium channel (CHEMBL2095229)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Crystal structures and pharmacologic activities of 1,4-dihydropyridine calcium channel antagonists of the isobutyl methyl 2,6-dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (nisoldipine) series.
Fossheim R, Joslyn A, Solo AJ, Luchowski E, Rutledge A, Triggle DJ.
J Med Chem (1988) 31 : 300 -305
PubMed 3339603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.72 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317044 1 10.89
CHEMBL441428 1 10.82
CHEMBL103806 1 10.57
CHEMBL321999 1 9.85
CHEMBL105444 1 9.60
CHEMBL319033 1 8.82
CHEMBL102498 1 8.64
CHEMBL318521 1 8.55
CHEMBL102907 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317044 IC50 = 0.013 nM 10.89
CHEMBL441428 IC50 = 0.015 nM 10.82
CHEMBL103806 IC50 = 0.027 nM 10.57
CHEMBL321999 IC50 = 0.14 nM 9.85
CHEMBL105444 IC50 = 0.25 nM 9.60
CHEMBL319033 IC50 = 1.5 nM 8.82
CHEMBL102498 IC50 = 2.3 nM 8.64
CHEMBL318521 IC50 = 2.8 nM 8.55
CHEMBL102907 IC50 = 0.0081 nM -