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Assay Detail

CHEMBL3821538

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Functional
Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction after 30 mins
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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
IC50 9 5.58 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818643 1 7.77
CHEMBL23 DILTIAZEM 4.0 1 6.96
CHEMBL3818880 1 5.45
CHEMBL3817876 1 5.32
CHEMBL3819606 1 5.01
CHEMBL3819349 1 4.99
CHEMBL3819185 1 4.93
CHEMBL3817893 1 4.91
CHEMBL3817895 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818643 IC50 = 17.0 nM 7.77
CHEMBL23 DILTIAZEM IC50 = 110.0 nM 6.96
CHEMBL3818880 IC50 = 3530.0 nM 5.45
CHEMBL3817876 IC50 = 4820.0 nM 5.32
CHEMBL3819606 IC50 = 9820.0 nM 5.01
CHEMBL3819349 IC50 = 10270.0 nM 4.99
CHEMBL3819185 IC50 = 11620.0 nM 4.93
CHEMBL3817893 IC50 = 12420.0 nM 4.91
CHEMBL3817895 IC50 = 14490.0 nM 4.84