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Assay Detail

CHEMBL4714754

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

Binding
Inhibition of human TRPC3 expressed in HEK293 cells assessed as inhibition of GSK170-induced current in absence of extracellular calcium by whole cell patch-clamp method
2
Total Activities
2
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

Short transient receptor potential channel 3 (CHEMBL2417348)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity.
Zhang S,Romero LO,Deng S,Wang J,Li Y,Yang L,Hamilton DJ,Miller DD,Liao FF,Cordero-Morales JF,Wu Z,Li W
ACS Med Chem Lett (2021) 12 : 572 -578
PubMed 33859797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.36 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761535 1 6.43
CHEMBL4177187 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761535 IC50 = 370.0 nM 6.43
CHEMBL4177187 IC50 = 530.0 nM 6.28