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Assay Detail

CHEMBL866878

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

Functional
Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Alpha-methylated derivatives of 2-arachidonoyl glycerol: synthesis, CB1 receptor activity, and enzymatic stability.
Parkkari T, Myllymäki M, Savinainen JR, Saario SM, Castillo-Meléndez JA, Laitinen JT, Nevalainen T, Koskinen AM, Järvinen T.
Bioorg Med Chem Lett (2006) 16 : 2437 -2440
PubMed 16466915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.15 6.00
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122972 2-ARACHIDONOYLGLYCEROL 1 6.00
CHEMBL377180 1 5.00
CHEMBL381171 1 4.80
CHEMBL208282 1 4.80
CHEMBL205958 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122972 2-ARACHIDONOYLGLYCEROL EC50 = 1000.0 nM 6.00
CHEMBL377180 EC50 = 10000.0 nM 5.00
CHEMBL381171 EC50 = 15848.93 nM 4.80
CHEMBL208282 EC50 = 15848.93 nM 4.80
CHEMBL205958 Activity - -