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Assay Detail

CHEMBL1259269

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

Binding
Displacement of [3H]CP55940 from mouse spleen CB2 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Spleen
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL5373)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel 1',1'-chain substituted hexahydrocannabinols: 9β-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist.
Nikas SP, Alapafuja SO, Papanastasiou I, Paronis CA, Shukla VG, Papahatjis DP, Bowman AL, Halikhedkar A, Han X, Makriyannis A.
J Med Chem (2010) 53 : 6996 -7010
PubMed 20925434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.20 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1259244 1 9.01
CHEMBL1259038 1 8.80
CHEMBL1259092 1 8.78
CHEMBL2218896 NABILONE 4.0 1 8.74
CHEMBL1259037 1 8.59
CHEMBL1259056 1 8.56
CHEMBL1259091 1 8.56
CHEMBL1259076 1 8.38
CHEMBL1259243 1 8.28
CHEMBL1259057 1 8.12
CHEMBL1259001 1 7.92
CHEMBL1259018 1 7.86
CHEMBL1259019 1 7.86
CHEMBL1259075 1 7.86
CHEMBL1259000 1 7.37
CHEMBL1259227 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1259244 Ki = 0.97 nM 9.01
CHEMBL1259038 Ki = 1.6 nM 8.80
CHEMBL1259092 Ki = 1.67 nM 8.78
CHEMBL2218896 NABILONE Ki = 1.8 nM 8.74
CHEMBL1259037 Ki = 2.59 nM 8.59
CHEMBL1259056 Ki = 2.78 nM 8.56
CHEMBL1259091 Ki = 2.76 nM 8.56
CHEMBL1259076 Ki = 4.21 nM 8.38
CHEMBL1259243 Ki = 5.25 nM 8.28
CHEMBL1259057 Ki = 7.56 nM 8.12
CHEMBL1259001 Ki = 12.0 nM 7.92
CHEMBL1259018 Ki = 13.7 nM 7.86
CHEMBL1259019 Ki = 13.9 nM 7.86
CHEMBL1259075 Ki = 13.9 nM 7.86
CHEMBL1259000 Ki = 42.3 nM 7.37
CHEMBL1259227 Ki = 265.0 nM 6.58