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Assay Detail

CHEMBL4809529

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

Binding
Inhibition of sodium channel (unknown origin) expressed in HEK cells assessed as reduction in late inward sodium current by automated patch clamp method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Antiarrhythmic Hit to Lead Refinement in a Dish Using Patient-Derived iPSC Cardiomyocytes.
Cashman JR, Ryan D, McKeithan WL, Okolotowicz K, Gomez-Galeno J, Johnson M, Sampson KJ, Kass RS, Pezhouman A, Karagueuzian HS, Mercola M.
J Med Chem (2021) 64 : 5384 -5403
PubMed 33942619 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.36 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862853 1 6.70
CHEMBL4850036 1 6.19
CHEMBL4851381 1 6.13
CHEMBL4851821 1 6.12
CHEMBL4875966 1 5.99
CHEMBL4875397 1 5.99
CHEMBL4876024 1 5.99
CHEMBL4872490 1 5.98
CHEMBL4860330 1 5.13
CHEMBL4853576 1 5.00
CHEMBL4741603 1 4.94
CHEMBL4742143 1 4.93
CHEMBL4848088 1 4.76
CHEMBL147507 (R)-MEXILETINE 1 4.72
CHEMBL558 MEXILETINE 4.0 1 4.65
CHEMBL146855 (S)-MEXILETINE 1 4.52
CHEMBL4855496 1 4.44
CHEMBL4867322 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862853 IC50 = 200.0 nM 6.70
CHEMBL4850036 IC50 = 643.0 nM 6.19
CHEMBL4851381 IC50 = 747.0 nM 6.13
CHEMBL4851821 IC50 = 753.0 nM 6.12
CHEMBL4875966 IC50 = 1030.0 nM 5.99
CHEMBL4875397 IC50 = 1030.0 nM 5.99
CHEMBL4876024 IC50 = 1020.0 nM 5.99
CHEMBL4872490 IC50 = 1040.0 nM 5.98
CHEMBL4860330 IC50 = 7400.0 nM 5.13
CHEMBL4853576 IC50 = 10000.0 nM 5.00
CHEMBL4741603 IC50 = 11400.0 nM 4.94
CHEMBL4742143 IC50 = 11700.0 nM 4.93
CHEMBL4848088 IC50 = 17300.0 nM 4.76
CHEMBL147507 (R)-MEXILETINE IC50 = 19000.0 nM 4.72
CHEMBL558 MEXILETINE IC50 = 22500.0 nM 4.65
CHEMBL146855 (S)-MEXILETINE IC50 = 29900.0 nM 4.52
CHEMBL4855496 IC50 = 36000.0 nM 4.44
CHEMBL4867322 IC50 = 51800.0 nM 4.29