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Assay Detail

CHEMBL4236332

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

Binding
Displacement of [3H]CP-55,940 from recombinant mouse Cb2 receptor expressed in HEK293 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Oximes short-acting CB1 receptor agonists.
Malamas MS, Raghav JG, Ma X, Honrao C, Wood JT, Benchama O, Zhou H, Mallipeddi S, Makriyannis A.
Bioorg Med Chem (2018) 26 : 4963 -4970
PubMed 30122284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.46 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4239190 1 10.00
CHEMBL4240671 1 9.30
CHEMBL4238224 1 8.82
CHEMBL4240996 1 8.80
CHEMBL4246445 1 8.74
CHEMBL4238778 1 8.72
CHEMBL4242964 1 8.60
CHEMBL4249273 1 8.59
CHEMBL4245472 1 8.55
CHEMBL58501 1 8.49
CHEMBL4249729 1 8.43
CHEMBL4237501 1 8.42
CHEMBL4243768 1 8.39
CHEMBL4239541 1 8.17
CHEMBL464679 1 7.39
CHEMBL4244186 1 7.36
CHEMBL4248866 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4239190 Ki = 0.1 nM 10.00
CHEMBL4240671 Ki = 0.5 nM 9.30
CHEMBL4238224 Ki = 1.5 nM 8.82
CHEMBL4240996 Ki = 1.6 nM 8.80
CHEMBL4246445 Ki = 1.8 nM 8.74
CHEMBL4238778 Ki = 1.9 nM 8.72
CHEMBL4242964 Ki = 2.5 nM 8.60
CHEMBL4249273 Ki = 2.6 nM 8.59
CHEMBL4245472 Ki = 2.8 nM 8.55
CHEMBL58501 Ki = 3.2 nM 8.49
CHEMBL4249729 Ki = 3.7 nM 8.43
CHEMBL4237501 Ki = 3.8 nM 8.42
CHEMBL4243768 Ki = 4.1 nM 8.39
CHEMBL4239541 Ki = 6.7 nM 8.17
CHEMBL464679 Ki = 40.4 nM 7.39
CHEMBL4244186 Ki = 43.6 nM 7.36
CHEMBL4248866 Ki = 74.8 nM 7.13