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Assay Detail

CHEMBL4201489

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

Binding
Displacement of [3H]CP-55,940 from human CB2 receptor expressed in HEK293 cell membranes in absence of FAAH inhibitor PMSF by radioligand binding assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 20 7.39 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215369 1 8.37
CHEMBL4206063 1 8.17
CHEMBL4213900 1 8.07
CHEMBL4206580 1 7.98
CHEMBL4218304 1 7.95
CHEMBL4213566 1 7.89
CHEMBL4218835 1 7.66
CHEMBL4208217 1 7.61
CHEMBL4216075 1 7.30
CHEMBL4211106 1 6.92
CHEMBL4210946 1 6.86
CHEMBL15848 ANANDAMIDE 1 6.80
CHEMBL4208628 1 6.75
CHEMBL4207686 1 6.73
CHEMBL120526 METHANANDAMIDE 1 6.66
CHEMBL4203180 1 6.54
CHEMBL4214829 1 -
CHEMBL4215534 1 -
CHEMBL4203857 1 -
CHEMBL4203343 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215369 Ki = 4.3 nM 8.37
CHEMBL4206063 Ki = 6.8 nM 8.17
CHEMBL4213900 Ki = 8.5 nM 8.07
CHEMBL4206580 Ki = 10.4 nM 7.98
CHEMBL4218304 Ki = 11.2 nM 7.95
CHEMBL4213566 Ki = 12.8 nM 7.89
CHEMBL4218835 Ki = 22.1 nM 7.66
CHEMBL4208217 Ki = 24.7 nM 7.61
CHEMBL4216075 Ki = 50.5 nM 7.30
CHEMBL4211106 Ki = 120.0 nM 6.92
CHEMBL4210946 Ki = 139.0 nM 6.86
CHEMBL15848 ANANDAMIDE Ki = 160.0 nM 6.80
CHEMBL4208628 Ki = 176.0 nM 6.75
CHEMBL4207686 Ki = 188.0 nM 6.73
CHEMBL120526 METHANANDAMIDE Ki = 220.0 nM 6.66
CHEMBL4203180 Ki = 286.0 nM 6.54
CHEMBL4214829 Ki > 1000.0 nM -
CHEMBL4215534 Ki > 1000.0 nM -
CHEMBL4203857 Ki > 1000.0 nM -
CHEMBL4203343 Ki > 1000.0 nM -