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Assay Detail

CHEMBL1099680

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Functional
Vasorelaxant activity in 80 mM K+-depolarized guinea pig thoracic aortic strip assessed as inhibition of calcium-induced contraction
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Aorta
Confidence 1 — Organism
Curated By Autocuration

Target

Aorta (CHEMBL613672)
Type TISSUE
Organism Cavia porcellus

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 5 5.09 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23 DILTIAZEM 4.0 1 5.58
CHEMBL1076181 1 5.29
CHEMBL1076546 1 5.25
CHEMBL213369 1 4.75
CHEMBL214488 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23 DILTIAZEM IC50 = 2600.0 nM 5.58
CHEMBL1076181 IC50 = 5160.0 nM 5.29
CHEMBL1076546 IC50 = 5620.0 nM 5.25
CHEMBL213369 IC50 = 17700.0 nM 4.75
CHEMBL214488 IC50 = 25100.0 nM 4.60