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Assay Detail

CHEMBL4201490

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

Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
12
Total Activities
12
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

( R)- N-(1-Methyl-2-hydroxyethyl)-13-( S)-methyl-arachidonamide (AMG315): A Novel Chiral Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes.
Liu Y, Ji L, Eno M, Kudalkar S, Li AL, Schimpgen M, Benchama O, Morales P, Xu S, Hurst D, Wu S, Mohammad KA, Wood JT, Zvonok N, Papahatjis DP, Zhou H, Honrao C, Mackie K, Reggio P, Hohmann AG, Marnett LJ, Makriyannis A, Nikas SP.
J Med Chem (2018) 61 : 8639 -8657
PubMed 30196704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.10 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215369 1 9.52
CHEMBL4208628 1 9.22
CHEMBL4213900 1 8.72
CHEMBL4208217 1 8.32
CHEMBL4218304 1 7.98
CHEMBL4216075 1 7.88
CHEMBL4213566 1 7.55
CHEMBL4206063 1 7.44
CHEMBL4211106 1 7.23
CHEMBL15848 ANANDAMIDE 1 7.16
CHEMBL4207686 1 -
CHEMBL4215534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215369 EC50 = 0.3 nM 9.52
CHEMBL4208628 EC50 = 0.6 nM 9.22
CHEMBL4213900 EC50 = 1.9 nM 8.72
CHEMBL4208217 EC50 = 4.8 nM 8.32
CHEMBL4218304 EC50 = 10.4 nM 7.98
CHEMBL4216075 EC50 = 13.2 nM 7.88
CHEMBL4213566 EC50 = 28.4 nM 7.55
CHEMBL4206063 EC50 = 36.1 nM 7.44
CHEMBL4211106 EC50 = 58.3 nM 7.23
CHEMBL15848 ANANDAMIDE EC50 = 69.0 nM 7.16
CHEMBL4207686 EC50 - -
CHEMBL4215534 EC50 - -