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Assay Detail

CHEMBL5536423

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

Functional
Agonist activity at rat CB1 receptor stably expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 5 mins by Lance Ultra cAMP assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chiral Me-2-arachidonoyl Glycerols: The First Potent Endocannabinoid Glyceride Templates with Stability to COX-2.
Nikas SP, Ji L, Liu Y, Georgiadis MO, Dopeshwarkar A, Straiker A, Kudalkar S, Sadybekov AV, Dvorakova M, Katritch V, Mackie K, Marnett L, Makriyannis A.
ACS Med Chem Lett (2024) 15 : 965 -971
PubMed 38894922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.85 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 8.46
CHEMBL5562759 1 8.15
CHEMBL5574568 1 7.77
CHEMBL5572923 1 7.64
CHEMBL122972 2-ARACHIDONOYLGLYCEROL 1 7.60
CHEMBL5573266 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 EC50 = 3.5 nM 8.46
CHEMBL5562759 EC50 = 7.0 nM 8.15
CHEMBL5574568 EC50 = 17.0 nM 7.77
CHEMBL5572923 EC50 = 23.1 nM 7.64
CHEMBL122972 2-ARACHIDONOYLGLYCEROL EC50 = 25.0 nM 7.60
CHEMBL5573266 EC50 = 34.6 nM 7.46