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Assay Detail

CHEMBL699700

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

Functional
Compound was evaluated for its effective dose to inhibit the calcium release as a measure of affinity for Inositol 1,4,5-trisphosphate receptor
3
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Inositol 1,4,5-trisphosphate receptor (CHEMBL2111451)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Total synthesis of L-2,2-difluoro-2-deoxy-MYO-inositol 1,4,5-trisphosphate, a potent inhibitor of the enzymes of d-MYO-inositol 1,4,5-trisphosphate metabolism
Sawyer DA, Potter BV
Bioorg Med Chem Lett (1991) 1 : 705 -710
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.85 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161456 1 6.89
CHEMBL1161466 2 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161456 EC50 = 130.0 nM 6.89
CHEMBL1161466 EC50 = 410.0 nM 6.39
CHEMBL1161466 EC50 = 53000.0 nM 4.28