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Assay Detail

CHEMBL706154

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

Binding
Inhibition of [3H](+)-PN200-110 binding to calcium channels of rat heart membranes.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL3762)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl(omega-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate iodide, calcium channel antagonists.
Peri R, Padmanabhan S, Rutledge A, Singh S, Triggle DJ.
J Med Chem (2000) 43 : 2906 -2914
PubMed 10956198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.13 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3350227 1 8.10
CHEMBL609701 1 7.00
CHEMBL2092919 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3350227 Ki = 8.0 nM 8.10
CHEMBL609701 Ki = 99.2 nM 7.00
CHEMBL2092919 Ki = 497.0 nM 6.30