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Assay Detail

CHEMBL961829

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

Binding
Binding affinity to human recombinant CB2 receptor expressed in african green monkey COS cells by radioligand binding assay
43
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo.
Brizzi A, Brizzi V, Cascio MG, Corelli F, Guida F, Ligresti A, Maione S, Martinelli A, Pasquini S, Tuccinardi T, Di Marzo V.
J Med Chem (2009) 52 : 2506 -2514
PubMed 19331413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 6.89 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307696 1 9.82
CHEMBL188 WIN-552122 1 8.68
CHEMBL489251 2 8.10
CHEMBL490648 2 8.10
CHEMBL225506 1 7.89
CHEMBL489252 2 7.70
CHEMBL491658 2 7.52
CHEMBL484887 2 7.50
CHEMBL484888 2 7.50
CHEMBL490035 2 7.10
CHEMBL490245 2 6.92
CHEMBL521944 2 6.90
CHEMBL491862 2 6.80
CHEMBL490246 2 6.70
CHEMBL491065 2 6.70
CHEMBL519043 1 6.29
CHEMBL489622 2 6.24
CHEMBL483670 2 6.22
CHEMBL489834 2 5.80
CHEMBL489623 2 5.62
CHEMBL488933 1 5.30
CHEMBL522123 2 5.00
CHEMBL489835 2 5.00
CHEMBL490046 2 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307696 Ki = 0.15 nM 9.82
CHEMBL188 WIN-552122 Ki = 2.1 nM 8.68
CHEMBL489251 Ki = 7.943 nM 8.10
CHEMBL490648 Ki = 7.9 nM 8.10
CHEMBL489251 Ki = 7.9 nM 8.10
CHEMBL490648 Ki = 7.943 nM 8.10
CHEMBL225506 Ki = 13.0 nM 7.89
CHEMBL489252 Ki = 20.0 nM 7.70
CHEMBL489252 Ki = 19.95 nM 7.70
CHEMBL491658 Ki = 30.0 nM 7.52
CHEMBL491658 Ki = 31.62 nM 7.50
CHEMBL484887 Ki = 31.62 nM 7.50
CHEMBL484888 Ki = 31.62 nM 7.50
CHEMBL484887 Ki = 34.0 nM 7.47
CHEMBL484888 Ki = 35.0 nM 7.46
CHEMBL490035 Ki = 79.43 nM 7.10
CHEMBL490035 Ki = 80.0 nM 7.10
CHEMBL490245 Ki = 120.0 nM 6.92
CHEMBL521944 Ki = 125.89 nM 6.90
CHEMBL490245 Ki = 125.89 nM 6.90
CHEMBL521944 Ki = 130.0 nM 6.89
CHEMBL491862 Ki = 160.0 nM 6.80
CHEMBL491862 Ki = 158.49 nM 6.80
CHEMBL491065 Ki = 200.0 nM 6.70
CHEMBL491065 Ki = 199.53 nM 6.70
CHEMBL490246 Ki = 199.53 nM 6.70
CHEMBL490246 Ki = 210.0 nM 6.68
CHEMBL519043 Ki = 510.0 nM 6.29
CHEMBL489622 Ki = 570.0 nM 6.24
CHEMBL483670 Ki = 600.0 nM 6.22
CHEMBL483670 Ki = 630.96 nM 6.20
CHEMBL489622 Ki = 630.96 nM 6.20
CHEMBL489834 Ki = 1584.89 nM 5.80
CHEMBL489834 Ki = 1620.0 nM 5.79
CHEMBL489623 Ki = 2420.0 nM 5.62
CHEMBL489623 Ki = 2511.89 nM 5.60
CHEMBL488933 Ki = 5000.0 nM 5.30
CHEMBL490046 Ki = 10000.0 nM 5.00
CHEMBL489835 Ki = 10000.0 nM 5.00
CHEMBL522123 Ki = 10000.0 nM 5.00
CHEMBL522123 Ki - -
CHEMBL490046 Ki - -
CHEMBL489835 Ki - -