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Assay Detail

CHEMBL4714699

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

Binding
Inhibition of SOCE channel in tBhQ-treated HEK cells assessed as reduction in calcium entry preincubated for 600 secs followed by calcium addition by Fura-2 AM by fluorescence microscopic analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry.
Aprile S,Riva B,Bhela IP,Cordero-Sanchez C,Avino G,Genazzani AA,Serafini M,Pirali T
ACS Med Chem Lett (2021) 12 : 640 -646
PubMed 33854704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.52 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3403742 1 6.70
CHEMBL4177187 1 6.30
CHEMBL4800501 1 5.51
CHEMBL4172741 1 5.36
CHEMBL4764577 1 5.26
CHEMBL4785581 1 5.02
CHEMBL4764376 1 5.02
CHEMBL4746984 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3403742 IC50 = 200.0 nM 6.70
CHEMBL4177187 IC50 = 500.0 nM 6.30
CHEMBL4800501 IC50 = 3100.0 nM 5.51
CHEMBL4172741 IC50 = 4400.0 nM 5.36
CHEMBL4764577 IC50 = 5500.0 nM 5.26
CHEMBL4785581 IC50 = 9500.0 nM 5.02
CHEMBL4764376 IC50 = 9600.0 nM 5.02
CHEMBL4746984 IC50 = 9700.0 nM 5.01