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Assay Detail

CHEMBL4377100

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Binding
Inhibition of YFP-tagged TRPC3 (unknown origin) expressed in HEK293 cells assessed as reduction carbhocol-induced receptor operated Calcium influx after 5 mins by fura-2-AM dye based assay
4
Total Activities
4
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

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 4 5.63 6.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177187 1 6.27
CHEMBL4460029 1 6.14
CHEMBL262766 1 5.38
CHEMBL101896 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177187 IC50 = 540.0 nM 6.27
CHEMBL4460029 IC50 = 720.0 nM 6.14
CHEMBL262766 IC50 = 4210.0 nM 5.38
CHEMBL101896 IC50 = 18460.0 nM 4.73