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Assay Detail

CHEMBL934086

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

Binding
Activity at L type calcium channel in K+ depolarized guinea pig longitudinal smooth muscle assessed as inhibition of calcium induced contraction
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity.
Budriesi R, Ioan P, Locatelli A, Cosconati S, Leoni A, Ugenti MP, Andreani A, Di Toro R, Bedini A, Spampinato S, Marinelli L, Novellino E, Chiarini A.
J Med Chem (2008) 51 : 1592 -1600
PubMed 18303827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.13 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193 NIFEDIPINE 4.0 1 8.82
CHEMBL271355 1 7.26
CHEMBL411235 1 7.08
CHEMBL439315 1 6.62
CHEMBL405876 1 6.26
CHEMBL272471 1 5.78
CHEMBL409148 1 5.71
CHEMBL271964 1 5.69
CHEMBL271993 1 5.59
CHEMBL271994 1 4.96
CHEMBL438024 1 4.91
CHEMBL412260 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193 NIFEDIPINE IC50 = 1.5 nM 8.82
CHEMBL271355 IC50 = 55.0 nM 7.26
CHEMBL411235 IC50 = 83.0 nM 7.08
CHEMBL439315 IC50 = 240.0 nM 6.62
CHEMBL405876 IC50 = 550.0 nM 6.26
CHEMBL272471 IC50 = 1660.0 nM 5.78
CHEMBL409148 IC50 = 1950.0 nM 5.71
CHEMBL271964 IC50 = 2060.0 nM 5.69
CHEMBL271993 IC50 = 2560.0 nM 5.59
CHEMBL271994 IC50 = 11040.0 nM 4.96
CHEMBL438024 IC50 = 12350.0 nM 4.91
CHEMBL412260 IC50 = 12810.0 nM 4.89