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Assay Detail

CHEMBL1030616

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

Binding
Displacement of [3H]CP-55940 from human cloned CB2 receptor by scintillation spectrometry
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 37 7.28 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL515090 1 8.77
CHEMBL516388 1 8.41
CHEMBL474897 1 8.28
CHEMBL475093 1 8.24
CHEMBL516057 1 8.03
CHEMBL474692 1 7.96
CHEMBL471671 1 7.96
CHEMBL514490 1 7.85
CHEMBL515102 1 7.77
CHEMBL474896 1 7.64
CHEMBL472856 1 7.64
CHEMBL511150 1 7.64
CHEMBL500856 1 7.64
CHEMBL503518 1 7.57
CHEMBL258242 1 7.47
CHEMBL515866 1 7.46
CHEMBL474300 1 7.44
CHEMBL473063 1 7.32
CHEMBL472679 1 7.23
CHEMBL474080 1 7.12
CHEMBL508362 1 7.12
CHEMBL475719 1 7.09
CHEMBL475100 1 7.09
CHEMBL473697 1 7.07
CHEMBL514324 1 7.06
CHEMBL473698 1 7.00
CHEMBL470233 1 6.92
CHEMBL470231 1 6.92
CHEMBL472680 1 6.89
CHEMBL474506 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL515090 Ki = 1.7 nM 8.77
CHEMBL516388 Ki = 3.9 nM 8.41
CHEMBL474897 Ki = 5.2 nM 8.28
CHEMBL475093 Ki = 5.7 nM 8.24
CHEMBL516057 Ki = 9.4 nM 8.03
CHEMBL474692 Ki = 11.0 nM 7.96
CHEMBL471671 Ki = 11.0 nM 7.96
CHEMBL514490 Ki = 14.0 nM 7.85
CHEMBL515102 Ki = 17.0 nM 7.77
CHEMBL472856 Ki = 23.0 nM 7.64
CHEMBL500856 Ki = 23.0 nM 7.64
CHEMBL511150 Ki = 23.0 nM 7.64
CHEMBL474896 Ki = 23.0 nM 7.64
CHEMBL503518 Ki = 27.0 nM 7.57
CHEMBL258242 Ki = 34.0 nM 7.47
CHEMBL515866 Ki = 35.0 nM 7.46
CHEMBL474300 Ki = 36.0 nM 7.44
CHEMBL473063 Ki = 48.0 nM 7.32
CHEMBL472679 Ki = 59.0 nM 7.23
CHEMBL508362 Ki = 75.0 nM 7.12
CHEMBL474080 Ki = 75.0 nM 7.12
CHEMBL475719 Ki = 81.0 nM 7.09
CHEMBL475100 Ki = 82.0 nM 7.09
CHEMBL473697 Ki = 85.0 nM 7.07
CHEMBL514324 Ki = 87.0 nM 7.06
CHEMBL473698 Ki = 100.0 nM 7.00
CHEMBL470233 Ki = 120.0 nM 6.92
CHEMBL470231 Ki = 120.0 nM 6.92
CHEMBL472680 Ki = 130.0 nM 6.89
CHEMBL474506 Ki = 160.0 nM 6.80
CHEMBL516368 Ki = 170.0 nM 6.77
CHEMBL470232 Ki = 540.0 nM 6.27
CHEMBL525791 Ki = 660.0 nM 6.18
CHEMBL475493 Ki = 800.0 nM 6.10
CHEMBL475500 Ki = 2000.0 nM 5.70
CHEMBL516078 Ki = 2900.0 nM 5.54
CHEMBL473696 Ki > 5000.0 nM -