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Assay Detail

CHEMBL779978

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

Functional
Effective concentration causing half-maximal [Ca2+] release in rat hepatocytes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Hepatocyte
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Synthesis and Ca2+-mobilizing activity of purine-modified mimics of adenophostin A: a model for the adenophostin-Ins(1,4,5)P3 receptor interaction.
Rosenberg HJ, Riley AM, Laude AJ, Taylor CW, Potter BV.
J Med Chem (2003) 46 : 4860 -4871
PubMed 14584937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.55 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161267 1 7.89
CHEMBL1161266 1 7.89
CHEMBL1161269 1 7.85
CHEMBL1161270 1 7.72
CHEMBL1161268 1 7.72
CHEMBL1161273 1 7.60
CHEMBL1161271 1 7.47
CHEMBL1161272 1 7.09
CHEMBL279107 INS(1,4,5)P3 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161267 EC50 = 13.0 nM 7.89
CHEMBL1161266 EC50 = 13.0 nM 7.89
CHEMBL1161269 EC50 = 14.0 nM 7.85
CHEMBL1161270 EC50 = 19.0 nM 7.72
CHEMBL1161268 EC50 = 19.0 nM 7.72
CHEMBL1161273 EC50 = 25.0 nM 7.60
CHEMBL1161271 EC50 = 34.0 nM 7.47
CHEMBL1161272 EC50 = 82.0 nM 7.09
CHEMBL279107 INS(1,4,5)P3 EC50 = 185.0 nM 6.73