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Assay Detail

CHEMBL658955

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

Binding
Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293-EBNA
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
López-Rodríguez ML, Viso A, Ortega-Gutiérrez S, Lastres-Becker I, González S, Fernández-Ruiz J, Ramos JA.
J Med Chem (2001) 44 : 4505 -4508
PubMed 11741470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.14 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 9.82
CHEMBL188 WIN-552122 1 8.41
CHEMBL434778 1 7.17
CHEMBL417158 1 7.16
CHEMBL38293 1 -
CHEMBL284300 1 -
CHEMBL39878 1 -
CHEMBL36774 1 -
CHEMBL287788 1 -
CHEMBL39460 1 -
CHEMBL290716 1 -
CHEMBL287364 1 -
CHEMBL287130 1 -
CHEMBL431128 1 -
CHEMBL15848 ANANDAMIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 Ki = 0.15 nM 9.82
CHEMBL188 WIN-552122 Ki = 3.9 nM 8.41
CHEMBL434778 Ki = 67.0 nM 7.17
CHEMBL417158 Ki = 70.0 nM 7.16
CHEMBL38293 Ki > 1000.0 nM -
CHEMBL284300 Ki > 1000.0 nM -
CHEMBL39878 Ki > 1000.0 nM -
CHEMBL36774 Ki > 1000.0 nM -
CHEMBL287788 Ki > 1000.0 nM -
CHEMBL39460 Ki > 1000.0 nM -
CHEMBL290716 Ki > 1000.0 nM -
CHEMBL287364 Ki > 1000.0 nM -
CHEMBL287130 Ki > 1000.0 nM -
CHEMBL431128 Ki > 1000.0 nM -
CHEMBL15848 ANANDAMIDE Ki > 1000.0 nM -