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Assay Detail

CHEMBL4015193

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

Binding
Agonist activity at mouse TRPC6 expressed in HEK293 cells co-expressing Gq11-PLCbeta fused M5 receptor assessed as peak current changes at +80 mV by whole cell patch-clamp method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Short transient receptor potential channel 6 (CHEMBL1795081)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
Qu C, Ding M, Zhu Y, Lu Y, Du J, Miller M, Tian J, Zhu J, Xu J, Wen M, Er-Bu A, Wang J, Xiao Y, Wu M, McManus OB, Li M, Wu J, Luo HR, Cao Z, Shen B, Wang H, Zhu MX, Hong X.
J Med Chem (2017) 60 : 4680 -4692
PubMed 28395140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.71 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085233 1 6.05
CHEMBL4060387 1 5.69
CHEMBL1496110 1 5.60
CHEMBL4060400 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085233 EC50 = 890.0 nM 6.05
CHEMBL4060387 EC50 = 2050.0 nM 5.69
CHEMBL1496110 EC50 = 2500.0 nM 5.60
CHEMBL4060400 EC50 = 3240.0 nM 5.49