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Assay Detail

CHEMBL5520039

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Binding
Antagonist activity at TRPC3 (unknown origin) assessed as inhibition of channel activity
5
Total Activities
5
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

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

Publication

Discovery of N-alkyl-N-benzyl thiazoles as novel TRPC antagonists for the treatment of glioblastoma multiforme.
Wang S, Li X, Hu Y, Wang L, Lv G, Feng Y, Sun Z, Cao Z, Liu Y, Wang H.
Eur J Med Chem (2024) 265 : 116066 -116066
PubMed 38185057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.41 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2418811 1 8.52
CHEMBL2418809 1 8.30
CHEMBL5558723 1 8.00
CHEMBL4177187 1 6.16
CHEMBL5532633 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2418811 IC50 = 3.0 nM 8.52
CHEMBL2418809 IC50 = 5.0 nM 8.30
CHEMBL5558723 IC50 = 10.0 nM 8.00
CHEMBL4177187 IC50 = 700.0 nM 6.16
CHEMBL5532633 IC50 = 840.0 nM 6.08