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Assay Detail

CHEMBL702008

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

Binding
Binding affinity against IP3 receptor in pig cerebellar membranes at a pH of 6.8 using [3H]Ins(1,4,5)P3 as the radioligand.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Cerebellum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type 1 InsP3 receptor isoform S2 (CHEMBL2950)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

The novel Ins(1,4,5)P3 analogue 3-amino-3-deoxy-Ins(1,4,5)P3: a pH-dependent Ins(1,4,5)P3 receptor partial agonist in SH-SY5Y neuroblastoma cells.
Kozikowski AP, Fauq AH, Wilcox RA, Challiss RA, Nahorski SR.
J Med Chem (1994) 37 : 868 -872
PubMed 8145238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.08 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1160022 1 7.11
CHEMBL1161529 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1160022 IC50 = 78.0 nM 7.11
CHEMBL1161529 IC50 = 9114.0 nM 5.04