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Assay Detail

CHEMBL1817475

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

Functional
Negative ionotropic activity against potassium-induced contraction in guinea pig left atrium assessed as decrease atrial rate
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines.
Budriesi R, Ioan P, Leoni A, Pedemonte N, Locatelli A, Micucci M, Chiarini A, Galietta LJ.
J Med Chem (2011) 54 : 3885 -3894
PubMed 21568323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.88 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1814700 1 8.66
CHEMBL44 GENISTEIN 2.0 1 7.55
CHEMBL1814699 1 7.54
CHEMBL1814583 1 7.51
CHEMBL1814576 1 7.48
CHEMBL1814701 1 7.47
CHEMBL1814575 1 6.92
CHEMBL193 NIFEDIPINE 4.0 1 6.58
CHEMBL1814577 1 6.57
CHEMBL1814582 1 6.47
CHEMBL1814581 1 6.41
CHEMBL1814584 1 6.37
CHEMBL1814579 1 6.14
CHEMBL1814574 1 5.97
CHEMBL1814578 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1814700 EC50 = 2.2 nM 8.66
CHEMBL44 GENISTEIN EC50 = 28.0 nM 7.55
CHEMBL1814699 EC50 = 29.0 nM 7.54
CHEMBL1814583 EC50 = 31.0 nM 7.51
CHEMBL1814576 EC50 = 33.0 nM 7.48
CHEMBL1814701 EC50 = 34.0 nM 7.47
CHEMBL1814575 EC50 = 120.0 nM 6.92
CHEMBL193 NIFEDIPINE EC50 = 260.0 nM 6.58
CHEMBL1814577 EC50 = 270.0 nM 6.57
CHEMBL1814582 EC50 = 340.0 nM 6.47
CHEMBL1814581 EC50 = 390.0 nM 6.41
CHEMBL1814584 EC50 = 430.0 nM 6.37
CHEMBL1814579 EC50 = 730.0 nM 6.14
CHEMBL1814574 EC50 = 1070.0 nM 5.97
CHEMBL1814578 EC50 = 2330.0 nM 5.63