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Assay Detail

CHEMBL3367869

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

Binding
Inhibition of TASK-3 (unknown origin) expressed in HEK293 cells by QPatch assay
8
Total Activities
8
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

Target

Potassium channel subfamily K member 9 (CHEMBL2321614)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.
Flaherty DP, Simpson DS, Miller M, Maki BE, Zou B, Shi J, Wu M, McManus OB, Aubé J, Li M, Golden JE.
Bioorg Med Chem Lett (2014) 24 : 3968 -3973
PubMed 25017033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.08 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3187482 1 7.42
CHEMBL3182449 1 6.60
CHEMBL1310568 1 6.16
CHEMBL3182359 1 6.15
CHEMBL1081188 1 6.00
CHEMBL3182725 1 6.00
CHEMBL3183773 1 5.41
CHEMBL3187891 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3187482 IC50 = 38.0 nM 7.42
CHEMBL3182449 IC50 = 250.0 nM 6.60
CHEMBL1310568 IC50 = 690.0 nM 6.16
CHEMBL3182359 IC50 = 710.0 nM 6.15
CHEMBL1081188 IC50 = 990.0 nM 6.00
CHEMBL3182725 IC50 = 990.0 nM 6.00
CHEMBL3183773 IC50 = 3940.0 nM 5.41
CHEMBL3187891 IC50 = 12500.0 nM 4.90