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Assay Detail

CHEMBL1040884

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

Functional
Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
Frost JM, Dart MJ, Tietje KR, Garrison TR, Grayson GK, Daza AV, El-Kouhen OF, Yao BB, Hsieh GC, Pai M, Zhu CZ, Chandran P, Meyer MD.
J Med Chem (2010) 53 : 295 -315
PubMed 19921781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.05 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188 WIN-552122 1 8.00
CHEMBL271158 1 7.92
CHEMBL262865 1 6.61
CHEMBL576706 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188 WIN-552122 EC50 = 10.0 nM 8.00
CHEMBL271158 EC50 = 12.0 nM 7.92
CHEMBL262865 EC50 = 248.0 nM 6.61
CHEMBL576706 EC50 = 2077.0 nM 5.68