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Assay Detail

CHEMBL4426149

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Functional
Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method
16
Total Activities
8
Compounds Tested
2
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

Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.
Morales P, Gómez-Cañas M, Navarro G, Hurst DP, Carrillo-Salinas FJ, Lagartera L, Pazos R, Goya P, Reggio PH, Guaza C, Franco R, Fernández-Ruiz J, Jagerovic N.
J Med Chem (2016) 59 : 6753 -6771
PubMed 27309150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.04 7.41
Emax 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4444725 2 7.41
CHEMBL4585657 2 7.30
CHEMBL497392 2 7.19
CHEMBL4557358 2 7.02
CHEMBL4588694 2 6.27
CHEMBL4562832 2 -
CHEMBL559612 CP-55940 2 -
CHEMBL371214 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4444725 EC50 = 38.6 nM 7.41
CHEMBL4585657 EC50 = 50.2 nM 7.30
CHEMBL497392 EC50 = 64.5 nM 7.19
CHEMBL4557358 EC50 = 95.1 nM 7.02
CHEMBL4588694 EC50 = 539.6 nM 6.27
CHEMBL4562832 EC50 - -
CHEMBL559612 CP-55940 EC50 - -
CHEMBL371214 EC50 - -
CHEMBL4557358 Emax = 110.0 % -
CHEMBL4562832 Emax - -
CHEMBL4585657 Emax = 114.0 % -
CHEMBL4444725 Emax = 98.0 % -
CHEMBL4588694 Emax = 96.0 % -
CHEMBL559612 CP-55940 Emax - -
CHEMBL371214 Emax - -
CHEMBL497392 Emax = 91.0 % -