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Assay Detail

CHEMBL867179

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

Functional
Agonistic potency at rat IP3 type 1 receptor expressed in chicken DT40 cells
11
Total Activities
11
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 Expert

Target

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

Publication

A systematic study of C-glucoside trisphosphates as myo-inositol trisphosphate receptor ligands. Synthesis of beta-C-glucoside trisphosphates based on the conformational restriction strategy.
Terauchi M, Abe H, Tovey SC, Dedos SG, Taylor CW, Paul M, Trusselle M, Potter BV, Matsuda A, Shuto S.
J Med Chem (2006) 49 : 1900 -1909
PubMed 16539376 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.13 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204385 ADENOPHOSTIN A 1 8.68
CHEMBL383049 1 8.40
CHEMBL379040 1 8.34
CHEMBL382185 1 7.95
CHEMBL279107 INS(1,4,5)P3 1 7.61
CHEMBL205008 1 7.31
CHEMBL380941 1 6.67
CHEMBL204253 1 6.41
CHEMBL383659 1 5.97
CHEMBL204903 1 5.69
CHEMBL205303 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204385 ADENOPHOSTIN A EC50 = 2.1 nM 8.68
CHEMBL383049 EC50 = 4.0 nM 8.40
CHEMBL379040 EC50 = 4.6 nM 8.34
CHEMBL382185 EC50 = 11.3 nM 7.95
CHEMBL279107 INS(1,4,5)P3 EC50 = 24.8 nM 7.61
CHEMBL205008 EC50 = 49.2 nM 7.31
CHEMBL380941 EC50 = 213.0 nM 6.67
CHEMBL204253 EC50 = 394.0 nM 6.41
CHEMBL383659 EC50 = 1080.0 nM 5.97
CHEMBL204903 EC50 = 2040.0 nM 5.69
CHEMBL205303 EC50 = 4430.0 nM 5.35