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Assay Detail

CHEMBL1926463

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

Binding
Displacement of [3H]CP55940 from human CB2 receptor expressed in human HEK293 cells
26
Total Activities
26
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

Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor.
Brizzi A, Cascio MG, Frosini M, Ligresti A, Aiello F, Biotti I, Brizzi V, Pertwee RG, Corelli F, Di Marzo V.
J Med Chem (2011) 54 : 8278 -8288
PubMed 22044209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 5.96 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188 WIN-552122 1 8.70
CHEMBL1923772 1 6.96
CHEMBL1923771 1 6.72
CHEMBL1923778 1 6.51
CHEMBL1923773 1 6.42
CHEMBL1923762 1 6.10
CHEMBL1923763 1 6.10
CHEMBL1923764 1 6.10
CHEMBL1923757 1 6.06
CHEMBL1923765 1 6.04
CHEMBL1923769 1 5.95
CHEMBL1923766 1 5.94
CHEMBL122972 2-ARACHIDONOYLGLYCEROL 1 5.85
CHEMBL1923774 1 5.78
CHEMBL1923761 1 5.75
CHEMBL1923760 1 5.75
CHEMBL1923770 1 5.62
CHEMBL1923777 1 5.32
CHEMBL1923756 1 5.10
CHEMBL1923775 1 5.10
CHEMBL1923759 1 5.10
CHEMBL1923758 1 5.10
CHEMBL1923776 1 4.98
CHEMBL1923767 1 -
CHEMBL1923768 1 -
CHEMBL146346 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188 WIN-552122 Ki = 2.0 nM 8.70
CHEMBL1923772 Ki = 110.0 nM 6.96
CHEMBL1923771 Ki = 190.0 nM 6.72
CHEMBL1923778 Ki = 310.0 nM 6.51
CHEMBL1923773 Ki = 380.0 nM 6.42
CHEMBL1923762 Ki = 790.0 nM 6.10
CHEMBL1923763 Ki = 790.0 nM 6.10
CHEMBL1923764 Ki = 800.0 nM 6.10
CHEMBL1923757 Ki = 870.0 nM 6.06
CHEMBL1923765 Ki = 910.0 nM 6.04
CHEMBL1923769 Ki = 1130.0 nM 5.95
CHEMBL1923766 Ki = 1160.0 nM 5.94
CHEMBL122972 2-ARACHIDONOYLGLYCEROL Ki = 1400.0 nM 5.85
CHEMBL1923774 Ki = 1670.0 nM 5.78
CHEMBL1923761 Ki = 1800.0 nM 5.75
CHEMBL1923760 Ki = 1800.0 nM 5.75
CHEMBL1923770 Ki = 2390.0 nM 5.62
CHEMBL1923777 Ki = 4820.0 nM 5.32
CHEMBL1923756 Ki = 7870.0 nM 5.10
CHEMBL1923775 Ki = 7910.0 nM 5.10
CHEMBL1923759 Ki = 7870.0 nM 5.10
CHEMBL1923758 Ki = 7870.0 nM 5.10
CHEMBL1923776 Ki = 10440.0 nM 4.98
CHEMBL1923767 Ki > 10000.0 nM -
CHEMBL1923768 Ki > 10000.0 nM -
CHEMBL146346 Ki > 3000.0 nM -