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Assay Detail

CHEMBL699736

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

Binding
Inhibitory concentration required to displace [3H]insP3 from Inositol 1,4,5-trisphosphate receptor of bovine adrenal cortex membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Adrenal cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Chemical synthesis and biological evaluation of 1d-1,2,4,5-InsP4 and its 3-fluorinated counterpart 1d-3-F-1,2,4,5-InsP4 potent 1d-1,4,5-InsP3-like calcium mobilizing analogues
Kozikowski AP, Fauq AH, Wilcox RA, Nahorski SR
Bioorg Med Chem Lett (1995) 5 : 1295 -1300
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.73 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279107 INS(1,4,5)P3 1 8.26
CHEMBL3349691 1 8.06
CHEMBL1159850 1 8.01
CHEMBL1159846 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279107 INS(1,4,5)P3 IC50 = 5.5 nM 8.26
CHEMBL3349691 IC50 = 8.7 nM 8.06
CHEMBL1159850 IC50 = 9.7 nM 8.01
CHEMBL1159846 IC50 = 268.8 nM 6.57