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Assay Detail

CHEMBL3436205

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

Functional
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
1
Total Activities
1
Compounds Tested
1
Activity Types
6
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Cell Type CHO
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Voltage-gated L-type calcium channel (CHEMBL2095229)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

MICE models: superior to the HERG model in predicting Torsade de Pointes.
Kramer J, Obejero-Paz CA, Myatt G, Kuryshev YA, Bruening-Wright A, Verducci JS, Brown AM.
Sci Rep (2013) 3 : 1 -7
PubMed 23812503 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.05 4.05

Assay Parameters

Parameter Type Value Units Text
CA_SOL_CONC CA_SOL_CONC 1.8 mM
DETECTION_METHOD DETECTION_METHOD - QPatch automated patch clamp
HOLDING_POTENTIAL HOLDING_POTENTIAL - -40
MEAS_VOLT MEAS_VOLT - mV
T1_PULSE T1_PULSE 150.0 ms
TEMP TEMP - Ambient

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL850 SPARFLOXACIN 4.0 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL850 SPARFLOXACIN IC50 = 88800.0 nM 4.05