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Assay Detail

CHEMBL4181843

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Binding
Inhibition of Cav3.3 (unknown origin)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Bezençon O, Heidmann B, Siegrist R, Stamm S, Richard S, Pozzi D, Corminboeuf O, Roch C, Kessler M, Ertel EA, Reymond I, Pfeifer T, de Kanter R, Toeroek-Schafroth M, Moccia LG, Mawet J, Moon R, Rey M, Capeleto B, Fournier E.
J Med Chem (2017) 60 : 9769 -9789
PubMed 29116786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.89 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45816 MIBEFRADIL 4.0 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45816 MIBEFRADIL IC50 = 130.0 nM 6.89