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Assay Detail

CHEMBL4358388

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

Binding
Agonist activity at rat IP3R1 expressed in human HEK cells assessed as increase in calcium release by Mag-fluo4 dye based assay
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 (CHEMBL2804)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

d-chiro-Inositol Ribophostin: A Highly Potent Agonist of d-myo-Inositol 1,4,5-Trisphosphate Receptors: Synthesis and Biological Activities.
Mills SJ, Rossi AM, Konieczny V, Bakowski D, Taylor CW, Potter BVL.
J Med Chem (2020) 63 : 3238 -3251
PubMed 32052631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.09 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4578747 2 7.57
CHEMBL4483666 2 7.28
CHEMBL204385 ADENOPHOSTIN A 2 6.81
CHEMBL279107 INS(1,4,5)P3 2 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4578747 EC50 = 27.0 nM 7.57
CHEMBL4578747 EC50 = 26.92 nM 7.57
CHEMBL4483666 EC50 = 52.0 nM 7.28
CHEMBL4483666 EC50 = 52.48 nM 7.28
CHEMBL204385 ADENOPHOSTIN A EC50 = 155.0 nM 6.81
CHEMBL204385 ADENOPHOSTIN A EC50 = 154.88 nM 6.81
CHEMBL279107 INS(1,4,5)P3 EC50 = 209.0 nM 6.68
CHEMBL279107 INS(1,4,5)P3 EC50 = 208.93 nM 6.68