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Assay Detail

CHEMBL1031455

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

Functional
Agonist activity at human cloned CB2 receptor assessed as stimulation of [35S]GTPgammaS binding
37
Total Activities
36
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

CB2 selective sulfamoyl benzamides: optimization of the amide functionality.
Goodman AJ, Ajello CW, Worm K, Le Bourdonnec B, Savolainen MA, O'Hare H, Cassel JA, Stabley GJ, Dehaven RN, Labuda CJ, Koblish M, Little PJ, Brogdon BL, Smith SA, Dolle RE.
Bioorg Med Chem Lett (2009) 19 : 309 -313
PubMed 19091565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 7.21 8.34
Emax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516388 1 8.34
CHEMBL515090 1 8.02
CHEMBL472856 2 7.96
CHEMBL475093 1 7.68
CHEMBL258242 1 7.68
CHEMBL474897 1 7.64
CHEMBL473063 1 7.60
CHEMBL511150 1 7.54
CHEMBL471671 1 7.51
CHEMBL515866 1 7.48
CHEMBL514490 1 7.38
CHEMBL474300 1 7.33
CHEMBL515102 1 7.31
CHEMBL516057 1 7.31
CHEMBL500856 1 7.24
CHEMBL503518 1 7.24
CHEMBL473697 1 7.19
CHEMBL472679 1 7.16
CHEMBL508362 1 7.11
CHEMBL475100 1 7.11
CHEMBL472680 1 6.96
CHEMBL474896 1 6.92
CHEMBL474080 1 6.92
CHEMBL473698 1 6.89
CHEMBL475719 1 6.89
CHEMBL474506 1 6.89
CHEMBL514324 1 6.72
CHEMBL470233 1 6.66
CHEMBL516368 1 6.41
CHEMBL474692 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516388 EC50 = 4.6 nM 8.34
CHEMBL515090 EC50 = 9.6 nM 8.02
CHEMBL472856 EC50 = 11.0 nM 7.96
CHEMBL258242 EC50 = 21.0 nM 7.68
CHEMBL475093 EC50 = 21.0 nM 7.68
CHEMBL474897 EC50 = 23.0 nM 7.64
CHEMBL473063 EC50 = 25.0 nM 7.60
CHEMBL511150 EC50 = 29.0 nM 7.54
CHEMBL471671 EC50 = 31.0 nM 7.51
CHEMBL515866 EC50 = 33.0 nM 7.48
CHEMBL514490 EC50 = 42.0 nM 7.38
CHEMBL474300 EC50 = 47.0 nM 7.33
CHEMBL515102 EC50 = 49.0 nM 7.31
CHEMBL516057 EC50 = 49.0 nM 7.31
CHEMBL500856 EC50 = 58.0 nM 7.24
CHEMBL503518 EC50 = 57.0 nM 7.24
CHEMBL473697 EC50 = 64.0 nM 7.19
CHEMBL472679 EC50 = 70.0 nM 7.16
CHEMBL508362 EC50 = 77.0 nM 7.11
CHEMBL475100 EC50 = 78.0 nM 7.11
CHEMBL472680 EC50 = 110.0 nM 6.96
CHEMBL474896 EC50 = 120.0 nM 6.92
CHEMBL474080 EC50 = 120.0 nM 6.92
CHEMBL474506 EC50 = 130.0 nM 6.89
CHEMBL475719 EC50 = 130.0 nM 6.89
CHEMBL473698 EC50 = 130.0 nM 6.89
CHEMBL514324 EC50 = 190.0 nM 6.72
CHEMBL470233 EC50 = 220.0 nM 6.66
CHEMBL516368 EC50 = 390.0 nM 6.41
CHEMBL474692 EC50 = 8400.0 nM 5.08
CHEMBL470231 EC50 - -
CHEMBL470232 EC50 - -
CHEMBL516078 EC50 - -
CHEMBL525791 EC50 - -
CHEMBL475500 EC50 - -
CHEMBL473696 EC50 - -
CHEMBL472856 Emax = 84.0 % -