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Assay Detail

CHEMBL4158684

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

Binding
Inhibition of STIM1/STIM2/Orai1 (unknown origin) expressed in mouse BV2 cells assessed as reduction of store-operated calcium entry at 100 uM preincubated for 30 mins followed by tBhQ, mediated Ca2+ depletion and re-addition measured for 600 secs by Fluo-4 AM-based fluorometric assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Publication

Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis.
Riva B, Griglio A, Serafini M, Cordero-Sanchez C, Aprile S, Di Paola R, Gugliandolo E, Alansary D, Biocotino I, Lim D, Grosa G, Galli U, Niemeyer B, Sorba G, Canonico PL, Cuzzocrea S, Genazzani AA, Pirali T.
J Med Chem (2018) 61 : 9756 -9783
PubMed 30347159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.54 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177187 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177187 IC50 = 2900.0 nM 5.54