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Assay Detail

CHEMBL932402

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

Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
27
Total Activities
27
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 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.
Alig L, Alsenz J, Andjelkovic M, Bendels S, Bénardeau A, Bleicher K, Bourson A, David-Pierson P, Guba W, Hildbrand S, Kube D, Lübbers T, Mayweg AV, Narquizian R, Neidhart W, Nettekoven M, Plancher JM, Rocha C, Rogers-Evans M, Röver S, Schneider G, Taylor S, Waldmeier P.
J Med Chem (2008) 51 : 2115 -2127
PubMed 18335976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 7.94 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260625 1 8.92
CHEMBL410339 1 8.70
CHEMBL259654 1 8.70
CHEMBL408427 1 8.70
CHEMBL262857 1 8.52
CHEMBL409471 1 8.52
CHEMBL409217 1 8.40
CHEMBL263391 1 8.30
CHEMBL258753 1 8.30
CHEMBL258539 1 8.10
CHEMBL259656 1 7.96
CHEMBL410247 1 7.96
CHEMBL410248 1 7.58
CHEMBL409472 1 7.14
CHEMBL260810 1 6.81
CHEMBL409441 1 6.33
CHEMBL260284 1 6.11
CHEMBL428257 1 -
CHEMBL405888 1 -
CHEMBL263390 1 -
CHEMBL263128 1 -
CHEMBL263129 1 -
CHEMBL259699 1 -
CHEMBL262858 1 -
CHEMBL411054 1 -
CHEMBL259425 1 -
CHEMBL259339 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260625 EC50 = 1.2 nM 8.92
CHEMBL410339 EC50 = 2.0 nM 8.70
CHEMBL259654 EC50 = 2.0 nM 8.70
CHEMBL408427 EC50 = 2.0 nM 8.70
CHEMBL262857 EC50 = 3.0 nM 8.52
CHEMBL409471 EC50 = 3.0 nM 8.52
CHEMBL409217 EC50 = 4.0 nM 8.40
CHEMBL263391 EC50 = 5.0 nM 8.30
CHEMBL258753 EC50 = 5.0 nM 8.30
CHEMBL258539 EC50 = 8.0 nM 8.10
CHEMBL259656 EC50 = 11.0 nM 7.96
CHEMBL410247 EC50 = 11.0 nM 7.96
CHEMBL410248 EC50 = 26.0 nM 7.58
CHEMBL409472 EC50 = 72.0 nM 7.14
CHEMBL260810 EC50 = 156.0 nM 6.81
CHEMBL409441 EC50 = 466.0 nM 6.33
CHEMBL260284 EC50 = 784.0 nM 6.11
CHEMBL428257 EC50 - -
CHEMBL405888 EC50 - -
CHEMBL263390 EC50 - -
CHEMBL263128 EC50 - -
CHEMBL263129 EC50 - -
CHEMBL259699 EC50 - -
CHEMBL262858 EC50 - -
CHEMBL411054 EC50 - -
CHEMBL259425 EC50 - -
CHEMBL259339 EC50 - -