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Assay Detail

CHEMBL4377101

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

Binding
Inhibition of ORAI/STIM1 in thapsigargin treated rat RBL2H3 cells assessed as reduction in store-operated calcium entry after 5 mins by fura-2-AM dye based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

ORAI1/STIM1 (CHEMBL3832645)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
Sharma S, Hopkins CR.
J Med Chem (2019) 62 : 7589 -7602
PubMed 30943030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.92 6.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101896 1 6.31
CHEMBL4177187 1 6.27
CHEMBL262766 1 6.23
CHEMBL4460029 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101896 IC50 = 490.0 nM 6.31
CHEMBL4177187 IC50 = 540.0 nM 6.27
CHEMBL262766 IC50 = 590.0 nM 6.23
CHEMBL4460029 IC50 = 13080.0 nM 4.88