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Assay Detail

CHEMBL3855331

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

Binding
Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.
Remen L, Bezençon O, Simons L, Gaston R, Downing D, Gatfield J, Roch C, Kessler M, Mosbacher J, Pfeifer T, Grisostomi C, Rey M, Ertel EA, Moon R.
J Med Chem (2016) 59 : 8398 -8411
PubMed 27579577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.96 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1684950 SUVECALTAMIDE 2.0 1 8.92
CHEMBL3892579 1 7.54
CHEMBL3934636 ULIXACALTAMIDE 1.0 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1684950 SUVECALTAMIDE IC50 = 1.2 nM 8.92
CHEMBL3892579 IC50 = 29.0 nM 7.54
CHEMBL3934636 ULIXACALTAMIDE IC50 = 37.0 nM 7.43