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Assay Detail

CHEMBL700080

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

Binding
Inhibition of [3H]-isradipine binding to L-type [Ca2+] channel of rat brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
van Rhee AM, Jiang JL, Melman N, Olah ME, Stiles GL, Jacobson KA.
J Med Chem (1996) 39 : 2980 -2989
PubMed 8709132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.34 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2051956 DEXNIGULDIPINE 2.0 1 7.22
CHEMBL2112411 1 6.16
CHEMBL102138 1 6.04
CHEMBL100646 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2051956 DEXNIGULDIPINE Ki = 59.7 nM 7.22
CHEMBL2112411 Ki = 694.0 nM 6.16
CHEMBL102138 Ki = 910.0 nM 6.04
CHEMBL100646 Ki = 1170.0 nM 5.93