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Assay Detail

CHEMBL4015195

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

Binding
Agonist activity at human TRPC7 expressed in HEK293 cells assessed as increase in intracellular calcium level measured for 2.5 mins in presence of 2 mM Ca2+ by Fluo8-AM dye-based fluorescence 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 7 (CHEMBL4105799)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.63 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085233 1 7.05
CHEMBL4060387 1 6.67
CHEMBL4060400 1 6.50
CHEMBL1496110 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085233 EC50 = 90.0 nM 7.05
CHEMBL4060387 EC50 = 213.0 nM 6.67
CHEMBL4060400 EC50 = 314.0 nM 6.50
CHEMBL1496110 EC50 = 497.0 nM 6.30