Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2034643

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

Functional
Agonist activity at rat IP3R1 expressed in chicken DT40 cells assessed as induction of Ca2+ release
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type DT40
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

Contribution of phosphates and adenine to the potency of adenophostins at the IP₃ receptor: synthesis of all possible bisphosphates of adenophostin A.
Sureshan KM, Riley AM, Thomas MP, Tovey SC, Taylor CW, Potter BV.
J Med Chem (2012) 55 : 1706 -1720
PubMed 22248345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.18 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204385 ADENOPHOSTIN A 1 8.55
CHEMBL279107 INS(1,4,5)P3 1 7.64
CHEMBL2030675 1 6.97
CHEMBL21825 1 5.06
CHEMBL2030678 1 4.60
CHEMBL2030676 1 4.28
CHEMBL2030677 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204385 ADENOPHOSTIN A EC50 = 2.8 nM 8.55
CHEMBL279107 INS(1,4,5)P3 EC50 = 23.0 nM 7.64
CHEMBL2030675 EC50 = 107.0 nM 6.97
CHEMBL21825 EC50 = 8634.0 nM 5.06
CHEMBL2030678 EC50 = 25190.0 nM 4.60
CHEMBL2030676 EC50 = 53030.0 nM 4.28
CHEMBL2030677 EC50 - -