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Assay Detail

CHEMBL994489

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cell membrane
18
Total Activities
14
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

Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Appendino G, Ligresti A, Minassi A, Cascio MG, Allarà M, Taglialatela-Scafati O, Pertwee RG, De Petrocellis L, Di Marzo V.
J Med Chem (2009) 52 : 3001 -3009
PubMed 19361197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.33 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL474488 2 6.82
CHEMBL15848 ANANDAMIDE 1 6.78
CHEMBL485368 1 6.72
CHEMBL475904 2 6.72
CHEMBL485369 1 6.54
CHEMBL472661 2 6.47
CHEMBL472662 2 6.42
CHEMBL483143 1 5.79
CHEMBL483144 1 5.62
CHEMBL417675 PALMIDROL 3.0 1 -
CHEMBL280065 OLEOYLETHANOLAMIDE 1 -
CHEMBL484344 1 -
CHEMBL485197 1 -
CHEMBL294199 CAPSAICIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL474488 Ki = 150.0 nM 6.82
CHEMBL15848 ANANDAMIDE Ki = 168.0 nM 6.78
CHEMBL485368 Ki = 190.0 nM 6.72
CHEMBL475904 Ki = 190.0 nM 6.72
CHEMBL474488 Ki = 200.0 nM 6.70
CHEMBL475904 Ki = 240.0 nM 6.62
CHEMBL485369 Ki = 290.0 nM 6.54
CHEMBL472661 Ki = 340.0 nM 6.47
CHEMBL472662 Ki = 380.0 nM 6.42
CHEMBL483143 Ki = 1630.0 nM 5.79
CHEMBL472661 Ki = 2040.0 nM 5.69
CHEMBL483144 Ki = 2420.0 nM 5.62
CHEMBL472662 Ki = 4410.0 nM 5.36
CHEMBL417675 PALMIDROL Ki > 5000.0 nM -
CHEMBL280065 OLEOYLETHANOLAMIDE Ki > 10000.0 nM -
CHEMBL484344 Ki > 10000.0 nM -
CHEMBL485197 Ki > 10000.0 nM -
CHEMBL294199 CAPSAICIN Ki > 10000.0 nM -