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Assay Detail

CHEMBL1030615

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

Binding
Displacement of [3H]CP-55940 from human cloned CB1 receptor by scintillation spectrometry
34
Total Activities
34
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 1 (CHEMBL218)
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 34 6.18 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516388 1 6.89
CHEMBL515102 1 6.89
CHEMBL473697 1 6.85
CHEMBL474897 1 6.70
CHEMBL475093 1 6.58
CHEMBL472679 1 6.57
CHEMBL470233 1 6.57
CHEMBL503518 1 6.51
CHEMBL258242 1 6.51
CHEMBL474896 1 6.41
CHEMBL511150 1 6.33
CHEMBL508362 1 6.29
CHEMBL473698 1 6.28
CHEMBL473063 1 6.27
CHEMBL475100 1 6.25
CHEMBL515090 1 6.19
CHEMBL472680 1 6.13
CHEMBL474080 1 6.12
CHEMBL475719 1 6.11
CHEMBL474692 1 6.10
CHEMBL516368 1 5.96
CHEMBL500856 1 5.96
CHEMBL474300 1 5.96
CHEMBL516057 1 5.92
CHEMBL471671 1 5.92
CHEMBL515866 1 5.92
CHEMBL514324 1 5.85
CHEMBL514490 1 5.75
CHEMBL470231 1 5.72
CHEMBL525791 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516388 Ki = 130.0 nM 6.89
CHEMBL515102 Ki = 130.0 nM 6.89
CHEMBL473697 Ki = 140.0 nM 6.85
CHEMBL474897 Ki = 200.0 nM 6.70
CHEMBL475093 Ki = 260.0 nM 6.58
CHEMBL472679 Ki = 270.0 nM 6.57
CHEMBL470233 Ki = 270.0 nM 6.57
CHEMBL503518 Ki = 310.0 nM 6.51
CHEMBL258242 Ki = 310.0 nM 6.51
CHEMBL474896 Ki = 390.0 nM 6.41
CHEMBL511150 Ki = 470.0 nM 6.33
CHEMBL508362 Ki = 510.0 nM 6.29
CHEMBL473698 Ki = 530.0 nM 6.28
CHEMBL473063 Ki = 540.0 nM 6.27
CHEMBL475100 Ki = 560.0 nM 6.25
CHEMBL515090 Ki = 640.0 nM 6.19
CHEMBL472680 Ki = 740.0 nM 6.13
CHEMBL474080 Ki = 750.0 nM 6.12
CHEMBL475719 Ki = 770.0 nM 6.11
CHEMBL474692 Ki = 790.0 nM 6.10
CHEMBL516368 Ki = 1100.0 nM 5.96
CHEMBL500856 Ki = 1100.0 nM 5.96
CHEMBL474300 Ki = 1100.0 nM 5.96
CHEMBL516057 Ki = 1200.0 nM 5.92
CHEMBL471671 Ki = 1200.0 nM 5.92
CHEMBL515866 Ki = 1200.0 nM 5.92
CHEMBL514324 Ki = 1400.0 nM 5.85
CHEMBL514490 Ki = 1800.0 nM 5.75
CHEMBL470231 Ki = 1900.0 nM 5.72
CHEMBL525791 Ki = 2900.0 nM 5.54
CHEMBL472856 Ki = 3400.0 nM 5.47
CHEMBL474506 Ki = 6990.0 nM 5.16
CHEMBL473696 Ki > 5000.0 nM -
CHEMBL475493 Ki > 1000.0 nM -