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Assay Detail

CHEMBL4377055

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

Binding
Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced membrane potential by FMP-2 dye based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Short transient receptor potential channel 4 (CHEMBL1741219)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
Sharma S, Hopkins CR.
J Med Chem (2019) 62 : 7589 -7602
PubMed 30943030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.18 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436705 1 5.39
CHEMBL2396913 1 5.37
CHEMBL4438838 1 5.28
CHEMBL4440241 1 5.26
CHEMBL1376358 1 4.99
CHEMBL2396911 1 4.99
CHEMBL2396912 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436705 IC50 = 4100.0 nM 5.39
CHEMBL2396913 IC50 = 4300.0 nM 5.37
CHEMBL4438838 IC50 = 5200.0 nM 5.28
CHEMBL4440241 IC50 = 5500.0 nM 5.26
CHEMBL1376358 IC50 = 10300.0 nM 4.99
CHEMBL2396911 IC50 = 10200.0 nM 4.99
CHEMBL2396912 IC50 = 11000.0 nM 4.96