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Assay Detail

CHEMBL970836

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

Binding
Displacement of [3H]diltiazem from L-type calcium channel in Sprague-Dawley rat cardiac myocytes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
Carosati E, Budriesi R, Ioan P, Ugenti MP, Frosini M, Fusi F, Corda G, Cosimelli B, Spinelli D, Chiarini A, Cruciani G.
J Med Chem (2008) 51 : 5552 -5565
PubMed 18754582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.72 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492668 1 6.35
CHEMBL864 CARBINOXAMINE 4.0 1 5.97
CHEMBL275742 DEXPROPRANOLOL 2.0 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492668 Ki = 450.0 nM 6.35
CHEMBL864 CARBINOXAMINE Ki = 1080.0 nM 5.97
CHEMBL275742 DEXPROPRANOLOL Ki = 14500.0 nM 4.84