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Assay Detail

CHEMBL819972

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

Binding
Displacement of [3H]nitrendipine from calcium channel receptors (CCRs)
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

Synthesis and in vitro cardiovascular activity of 4-aryl-2,3,3a,4-tetrahydro-1h-pyrrolo[2,1-c][1,4]benzothiazin-1-ones and 7-acetoxy-6-phenyl-7a,8,9,10-tetrahydropyrrolo [2,1,-d][1,5]benzothiazepin-10-one.
Campiani G, Garofalo A, Fiorini I, Nacci V, Botta M, Tafi A, Chiarini A, Budriesi R, Bruni G, Romeo M
Bioorg Med Chem Lett (1994) 4 : 1235 -1240
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.31 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23 DILTIAZEM 4.0 1 7.38
CHEMBL282448 1 5.81
CHEMBL21575 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23 DILTIAZEM IC50 = 42.0 nM 7.38
CHEMBL282448 IC50 = 1550.0 nM 5.81
CHEMBL21575 IC50 = 1800.0 nM 5.75