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Assay Detail

CHEMBL3821524

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Functional
Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension after 30 mins
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Left atrium (CHEMBL2367407)
Type TISSUE
Organism Cavia porcellus

Publication

Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
Carosati E, Cosimelli B, Ioan P, Severi E, Katneni K, Chiu FC, Saponara S, Fusi F, Frosini M, Matucci R, Micucci M, Chiarini A, Spinelli D, Budriesi R.
J Med Chem (2016) 59 : 3340 -3352
PubMed 26962886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.49 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818643 1 7.66
CHEMBL3819168 1 7.42
CHEMBL3818880 1 7.19
CHEMBL3819349 1 7.02
CHEMBL3817941 1 7.00
CHEMBL3819606 1 6.85
CHEMBL3819180 1 6.85
CHEMBL3819226 1 6.68
CHEMBL3819185 1 6.66
CHEMBL326076 1 6.64
CHEMBL3818560 1 6.64
CHEMBL3818275 1 6.55
CHEMBL3817893 1 6.50
CHEMBL3817895 1 6.41
CHEMBL3819645 1 6.39
CHEMBL3818473 1 6.37
CHEMBL3818043 1 6.32
CHEMBL116310 1 6.31
CHEMBL115919 1 6.28
CHEMBL3817892 1 6.19
CHEMBL3819433 1 6.18
CHEMBL23 DILTIAZEM 4.0 1 6.10
CHEMBL3818844 1 6.06
CHEMBL3819023 1 6.03
CHEMBL3817876 1 5.92
CHEMBL3818651 1 5.89
CHEMBL419405 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818643 EC50 = 22.0 nM 7.66
CHEMBL3819168 EC50 = 38.0 nM 7.42
CHEMBL3818880 EC50 = 64.0 nM 7.19
CHEMBL3819349 EC50 = 95.0 nM 7.02
CHEMBL3817941 EC50 = 100.0 nM 7.00
CHEMBL3819606 EC50 = 140.0 nM 6.85
CHEMBL3819180 EC50 = 140.0 nM 6.85
CHEMBL3819226 EC50 = 210.0 nM 6.68
CHEMBL3819185 EC50 = 220.0 nM 6.66
CHEMBL326076 EC50 = 230.0 nM 6.64
CHEMBL3818560 EC50 = 230.0 nM 6.64
CHEMBL3818275 EC50 = 280.0 nM 6.55
CHEMBL3817893 EC50 = 320.0 nM 6.50
CHEMBL3817895 EC50 = 390.0 nM 6.41
CHEMBL3819645 EC50 = 410.0 nM 6.39
CHEMBL3818473 EC50 = 430.0 nM 6.37
CHEMBL3818043 EC50 = 480.0 nM 6.32
CHEMBL116310 EC50 = 490.0 nM 6.31
CHEMBL115919 EC50 = 520.0 nM 6.28
CHEMBL3817892 EC50 = 650.0 nM 6.19
CHEMBL3819433 EC50 = 660.0 nM 6.18
CHEMBL23 DILTIAZEM EC50 = 790.0 nM 6.10
CHEMBL3818844 EC50 = 870.0 nM 6.06
CHEMBL3819023 EC50 = 930.0 nM 6.03
CHEMBL3817876 EC50 = 1190.0 nM 5.92
CHEMBL3818651 EC50 = 1290.0 nM 5.89
CHEMBL419405 EC50 = 6580.0 nM 5.18