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Assay Detail

CHEMBL924304

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Functional
Agonist activity at human CB2 receptor by GTPgamma[35S] assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 31 8.76 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250608 1 9.52
CHEMBL250809 1 9.30
CHEMBL401480 1 9.30
CHEMBL249024 1 9.22
CHEMBL400399 1 9.10
CHEMBL249025 1 9.10
CHEMBL250609 1 9.05
CHEMBL404211 1 8.82
CHEMBL188 WIN-552122 1 8.82
CHEMBL250493 1 8.77
CHEMBL250607 1 8.77
CHEMBL250808 1 8.57
CHEMBL399949 1 8.40
CHEMBL250026 1 8.30
CHEMBL250491 1 8.17
CHEMBL250427 1 7.87
CHEMBL250626 1 7.81
CHEMBL400887 1 -
CHEMBL249827 1 -
CHEMBL399248 1 -
CHEMBL399948 1 -
CHEMBL400051 1 -
CHEMBL399316 1 -
CHEMBL249383 1 -
CHEMBL249786 1 -
CHEMBL249992 1 -
CHEMBL399346 1 -
CHEMBL250194 1 -
CHEMBL250810 1 -
CHEMBL251003 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250608 EC50 = 0.3 nM 9.52
CHEMBL250809 EC50 = 0.5 nM 9.30
CHEMBL401480 EC50 = 0.5 nM 9.30
CHEMBL249024 EC50 = 0.6 nM 9.22
CHEMBL400399 EC50 = 0.8 nM 9.10
CHEMBL249025 EC50 = 0.8 nM 9.10
CHEMBL250609 EC50 = 0.9 nM 9.05
CHEMBL404211 EC50 = 1.5 nM 8.82
CHEMBL188 WIN-552122 EC50 = 1.5 nM 8.82
CHEMBL250493 EC50 = 1.7 nM 8.77
CHEMBL250607 EC50 = 1.7 nM 8.77
CHEMBL250808 EC50 = 2.7 nM 8.57
CHEMBL399949 EC50 = 4.0 nM 8.40
CHEMBL250026 EC50 = 5.0 nM 8.30
CHEMBL250491 EC50 = 6.7 nM 8.17
CHEMBL250427 EC50 = 13.5 nM 7.87
CHEMBL250626 EC50 = 15.6 nM 7.81
CHEMBL400887 EC50 - -
CHEMBL249827 EC50 - -
CHEMBL399248 EC50 - -
CHEMBL399948 EC50 - -
CHEMBL400051 EC50 - -
CHEMBL399316 EC50 - -
CHEMBL249383 EC50 - -
CHEMBL249786 EC50 - -
CHEMBL249992 EC50 - -
CHEMBL399346 EC50 - -
CHEMBL250194 EC50 - -
CHEMBL250810 EC50 - -
CHEMBL251003 EC50 - -
CHEMBL251004 EC50 - -