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Assay Detail

CHEMBL1099688

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

Binding
Blockade of L-type calcium channel in Wistar rat cardiomyocytes assessed as inhibition of peak L-type barium current by whole cell patch clamp method
4
Total Activities
3
Compounds Tested
2
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

Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
Carosati E, Budriesi R, Ioan P, Cruciani G, Fusi F, Frosini M, Saponara S, Gasparrini F, Ciogli A, Villani C, Stephens PJ, Devlin FJ, Spinelli D, Chiarini A.
J Med Chem (2009) 52 : 6637 -6648
PubMed 19831392 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.62 4.65
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1076181 1 4.65
CHEMBL1076546 2 4.63
CHEMBL212643 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1076181 IC50 = 22200.0 nM 4.65
CHEMBL1076546 IC50 = 23500.0 nM 4.63
CHEMBL212643 IC50 = 27100.0 nM 4.57
CHEMBL1076546 Inhibition - % -