Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4201487

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

Binding
Displacement of [3H]CP-55,940 from CB1 receptor in rat brain membranes in presence 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 Rattus norvegicus
Tissue Brain
Subcellular Membrane
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
Ki 20 7.86 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215369 1 8.82
CHEMBL4208217 1 8.77
CHEMBL4213566 1 8.66
CHEMBL4206580 1 8.41
CHEMBL4218304 1 8.37
CHEMBL4216075 1 8.32
CHEMBL4213900 1 8.20
CHEMBL4208628 1 8.05
CHEMBL4218835 1 7.81
CHEMBL4211106 1 7.67
CHEMBL4206063 1 7.64
CHEMBL120526 METHANANDAMIDE 1 7.43
CHEMBL15848 ANANDAMIDE 1 7.13
CHEMBL4210946 1 7.10
CHEMBL4203180 1 7.08
CHEMBL4207686 1 6.28
CHEMBL4214829 1 -
CHEMBL4215534 1 -
CHEMBL4203857 1 -
CHEMBL4203343 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215369 Ki = 1.5 nM 8.82
CHEMBL4208217 Ki = 1.7 nM 8.77
CHEMBL4213566 Ki = 2.2 nM 8.66
CHEMBL4206580 Ki = 3.9 nM 8.41
CHEMBL4218304 Ki = 4.3 nM 8.37
CHEMBL4216075 Ki = 4.8 nM 8.32
CHEMBL4213900 Ki = 6.3 nM 8.20
CHEMBL4208628 Ki = 8.9 nM 8.05
CHEMBL4218835 Ki = 15.6 nM 7.81
CHEMBL4211106 Ki = 21.4 nM 7.67
CHEMBL4206063 Ki = 23.1 nM 7.64
CHEMBL120526 METHANANDAMIDE Ki = 37.0 nM 7.43
CHEMBL15848 ANANDAMIDE Ki = 74.0 nM 7.13
CHEMBL4210946 Ki = 79.0 nM 7.10
CHEMBL4203180 Ki = 83.0 nM 7.08
CHEMBL4207686 Ki = 520.0 nM 6.28
CHEMBL4214829 Ki > 1000.0 nM -
CHEMBL4215534 Ki > 1000.0 nM -
CHEMBL4203857 Ki > 1000.0 nM -
CHEMBL4203343 Ki > 1000.0 nM -