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Assay Detail

CHEMBL4359064

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

Binding
Activation of recombinant human TREK1 I293A mutant expressed in HEK293T cells assessed as increase in K+ current amplitude by whole cell voltage clamp electrophysiological analysis
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

Target

Potassium channel subfamily K member 2 (CHEMBL2321615)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.
Qiu Y, Huang L, Fu J, Han C, Fang J, Liao P, Chen Z, Mo Y, Sun P, Liao D, Yang L, Wang J, Zhang Q, Liu J, Liu F, Liu T, Huang W, Yang H, Jiang R.
J Med Chem (2020) 63 : 3665 -3677
PubMed 32162512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.10 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4552751 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4552751 EC50 = 7980.0 nM 5.10