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Assay Detail

CHEMBL924302

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Binding
Binding affinity to human CB2 receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
Pagé D, Yang H, Brown W, Walpole C, Fleurent M, Fyfe M, Gaudreault F, St-Onge S.
Bioorg Med Chem Lett (2007) 17 : 6183 -6187
PubMed 17884494 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.42 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188 WIN-552122 1 8.54
CHEMBL401480 1 8.38
CHEMBL250809 1 8.20
CHEMBL250608 1 8.19
CHEMBL249025 1 8.15
CHEMBL249024 1 8.10
CHEMBL250609 1 8.05
CHEMBL404211 1 8.03
CHEMBL400399 1 7.96
CHEMBL250808 1 7.78
CHEMBL250493 1 7.76
CHEMBL250607 1 7.75
CHEMBL250626 1 7.75
CHEMBL399949 1 7.65
CHEMBL250491 1 7.65
CHEMBL250026 1 7.63
CHEMBL399346 1 7.56
CHEMBL399948 1 7.56
CHEMBL251004 1 7.43
CHEMBL249992 1 7.42
CHEMBL399316 1 7.36
CHEMBL249827 1 7.07
CHEMBL400051 1 7.05
CHEMBL249786 1 6.97
CHEMBL400887 1 6.97
CHEMBL250427 1 6.85
CHEMBL250194 1 6.67
CHEMBL249383 1 6.51
CHEMBL250810 1 6.03
CHEMBL251003 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188 WIN-552122 Ki = 2.9 nM 8.54
CHEMBL401480 Ki = 4.2 nM 8.38
CHEMBL250809 Ki = 6.3 nM 8.20
CHEMBL250608 Ki = 6.4 nM 8.19
CHEMBL249025 Ki = 7.0 nM 8.15
CHEMBL249024 Ki = 7.9 nM 8.10
CHEMBL250609 Ki = 8.9 nM 8.05
CHEMBL404211 Ki = 9.4 nM 8.03
CHEMBL400399 Ki = 11.1 nM 7.96
CHEMBL250808 Ki = 16.8 nM 7.78
CHEMBL250493 Ki = 17.5 nM 7.76
CHEMBL250607 Ki = 17.6 nM 7.75
CHEMBL250626 Ki = 17.9 nM 7.75
CHEMBL399949 Ki = 22.3 nM 7.65
CHEMBL250491 Ki = 22.3 nM 7.65
CHEMBL250026 Ki = 23.3 nM 7.63
CHEMBL399346 Ki = 27.8 nM 7.56
CHEMBL399948 Ki = 27.6 nM 7.56
CHEMBL251004 Ki = 37.0 nM 7.43
CHEMBL249992 Ki = 38.1 nM 7.42
CHEMBL399316 Ki = 44.2 nM 7.36
CHEMBL249827 Ki = 84.7 nM 7.07
CHEMBL400051 Ki = 88.1 nM 7.05
CHEMBL249786 Ki = 107.0 nM 6.97
CHEMBL400887 Ki = 106.0 nM 6.97
CHEMBL250427 Ki = 140.0 nM 6.85
CHEMBL250194 Ki = 216.0 nM 6.67
CHEMBL249383 Ki = 308.0 nM 6.51
CHEMBL250810 Ki = 935.0 nM 6.03
CHEMBL251003 Ki = 1982.0 nM 5.70
CHEMBL399248 Ki = 4724.0 nM 5.33