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Assay Detail

CHEMBL4377092

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Binding
Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay
6
Total Activities
6
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 5 (CHEMBL1250411)
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 6 5.65 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309490 GALANGIN 1 6.35
CHEMBL150 KAEMPFEROL 1.0 1 5.41
CHEMBL50 QUERCETIN 3.0 1 5.19
CHEMBL164 MYRICETIN 1 -
CHEMBL28 APIGENIN 1 -
CHEMBL151 LUTEOLIN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309490 GALANGIN IC50 = 450.0 nM 6.35
CHEMBL150 KAEMPFEROL IC50 = 3900.0 nM 5.41
CHEMBL50 QUERCETIN IC50 = 6500.0 nM 5.19
CHEMBL164 MYRICETIN IC50 > 10000.0 nM -
CHEMBL28 APIGENIN IC50 > 10000.0 nM -
CHEMBL151 LUTEOLIN IC50 > 10000.0 nM -