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Assay Detail

CHEMBL2383763

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

Functional
Negative chronotropic activity in guinea pig right atrium assessed as decrease in atrial rate
12
Total Activities
12
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

Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity.
Locatelli A, Cosconati S, Micucci M, Leoni A, Marinelli L, Bedini A, Ioan P, Spampinato SM, Novellino E, Chiarini A, Budriesi R.
J Med Chem (2013) 56 : 3866 -3877
PubMed 23586669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.35 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193 NIFEDIPINE 4.0 1 7.41
CHEMBL2381470 1 5.97
CHEMBL2381468 1 5.89
CHEMBL2381472 1 5.67
CHEMBL2381471 1 5.64
CHEMBL2381582 1 5.58
CHEMBL2381467 1 5.13
CHEMBL2381465 1 4.90
CHEMBL2381462 1 4.61
CHEMBL2381464 1 4.55
CHEMBL2381463 1 4.40
CHEMBL2381469 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193 NIFEDIPINE EC50 = 39.0 nM 7.41
CHEMBL2381470 EC50 = 1060.0 nM 5.97
CHEMBL2381468 EC50 = 1300.0 nM 5.89
CHEMBL2381472 EC50 = 2160.0 nM 5.67
CHEMBL2381471 EC50 = 2300.0 nM 5.64
CHEMBL2381582 EC50 = 2630.0 nM 5.58
CHEMBL2381467 EC50 = 7490.0 nM 5.13
CHEMBL2381465 EC50 = 12460.0 nM 4.90
CHEMBL2381462 EC50 = 24390.0 nM 4.61
CHEMBL2381464 EC50 = 28440.0 nM 4.55
CHEMBL2381463 EC50 = 39910.0 nM 4.40
CHEMBL2381469 EC50 = 40500.0 nM 4.39