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Assay Detail

CHEMBL932920

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

Functional
Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
Frost JM, Dart MJ, Tietje KR, Garrison TR, Grayson GK, Daza AV, El-Kouhen OF, Miller LN, Li L, Yao BB, Hsieh GC, Pai M, Zhu CZ, Chandran P, Meyer MD.
J Med Chem (2008) 51 : 1904 -1912
PubMed 18311894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 54 7.28 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271158 1 8.15
CHEMBL270955 1 8.15
CHEMBL259462 1 8.00
CHEMBL411674 1 8.00
CHEMBL262865 1 7.85
CHEMBL409491 1 7.82
CHEMBL272868 1 7.75
CHEMBL272176 1 7.68
CHEMBL410677 1 7.66
CHEMBL409669 1 7.43
CHEMBL406399 1 7.39
CHEMBL410655 1 7.35
CHEMBL271814 1 7.30
CHEMBL272882 1 7.21
CHEMBL259253 1 7.19
CHEMBL410313 1 7.14
CHEMBL408964 1 7.09
CHEMBL188 WIN-552122 1 7.07
CHEMBL410676 1 7.04
CHEMBL270546 1 6.87
CHEMBL271837 1 6.73
CHEMBL409647 1 6.65
CHEMBL1203961 1 6.64
CHEMBL259463 1 6.55
CHEMBL410842 1 6.42
CHEMBL306764 1 6.20
CHEMBL409537 1 -
CHEMBL411244 1 -
CHEMBL408430 1 -
CHEMBL271810 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271158 EC50 = 7.0 nM 8.15
CHEMBL270955 EC50 = 7.0 nM 8.15
CHEMBL411674 EC50 = 10.0 nM 8.00
CHEMBL259462 EC50 = 10.0 nM 8.00
CHEMBL262865 EC50 = 14.0 nM 7.85
CHEMBL409491 EC50 = 15.0 nM 7.82
CHEMBL272868 EC50 = 18.0 nM 7.75
CHEMBL272176 EC50 = 21.0 nM 7.68
CHEMBL410677 EC50 = 22.0 nM 7.66
CHEMBL409669 EC50 = 37.0 nM 7.43
CHEMBL406399 EC50 = 41.0 nM 7.39
CHEMBL410655 EC50 = 45.0 nM 7.35
CHEMBL271814 EC50 = 50.0 nM 7.30
CHEMBL272882 EC50 = 61.0 nM 7.21
CHEMBL259253 EC50 = 64.0 nM 7.19
CHEMBL410313 EC50 = 73.0 nM 7.14
CHEMBL408964 EC50 = 81.0 nM 7.09
CHEMBL188 WIN-552122 EC50 = 86.0 nM 7.07
CHEMBL410676 EC50 = 92.0 nM 7.04
CHEMBL270546 EC50 = 135.0 nM 6.87
CHEMBL271837 EC50 = 186.0 nM 6.73
CHEMBL409647 EC50 = 226.0 nM 6.65
CHEMBL1203961 EC50 = 227.0 nM 6.64
CHEMBL259463 EC50 = 280.0 nM 6.55
CHEMBL410842 EC50 = 383.0 nM 6.42
CHEMBL306764 EC50 = 634.0 nM 6.20
CHEMBL271527 EC50 > 10000.0 nM -
CHEMBL409265 EC50 > 10000.0 nM -
CHEMBL272876 EC50 > 10000.0 nM -
CHEMBL406918 EC50 > 10000.0 nM -
CHEMBL411631 EC50 > 10000.0 nM -
CHEMBL269851 EC50 > 10000.0 nM -
CHEMBL411937 EC50 > 10000.0 nM -
CHEMBL411888 EC50 > 10000.0 nM -
CHEMBL270082 EC50 > 10000.0 nM -
CHEMBL408174 EC50 > 10000.0 nM -
CHEMBL411673 EC50 > 10000.0 nM -
CHEMBL272659 EC50 > 10000.0 nM -
CHEMBL409537 EC50 > 10000.0 nM -
CHEMBL410441 EC50 > 10000.0 nM -
CHEMBL271839 EC50 > 10000.0 nM -
CHEMBL271838 EC50 > 10000.0 nM -
CHEMBL272658 EC50 > 10000.0 nM -
CHEMBL271553 EC50 > 10000.0 nM -
CHEMBL271805 EC50 > 10000.0 nM -
CHEMBL272189 EC50 > 10000.0 nM -
CHEMBL270968 EC50 > 10000.0 nM -
CHEMBL271810 EC50 > 10000.0 nM -
CHEMBL408430 EC50 > 10000.0 nM -
CHEMBL411244 EC50 > 10000.0 nM -