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Assay Detail

CHEMBL4426148

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Functional
Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins by HTRF assay
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
IC50 8 7.65 8.38
Emax 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4444725 2 8.38
CHEMBL559612 CP-55940 2 8.08
CHEMBL4588694 2 7.85
CHEMBL4557358 2 7.67
CHEMBL4562832 2 7.59
CHEMBL371214 2 7.09
CHEMBL4585657 2 6.87
CHEMBL497392 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4444725 IC50 = 4.2 nM 8.38
CHEMBL559612 CP-55940 IC50 = 8.3 nM 8.08
CHEMBL4588694 IC50 = 14.0 nM 7.85
CHEMBL4557358 IC50 = 21.6 nM 7.67
CHEMBL4562832 IC50 = 25.5 nM 7.59
CHEMBL371214 IC50 = 81.8 nM 7.09
CHEMBL4585657 IC50 = 134.0 nM 6.87
CHEMBL497392 IC50 - -
CHEMBL4557358 Emax = 95.0 % -
CHEMBL4562832 Emax = 98.0 % -
CHEMBL4585657 Emax = 98.0 % -
CHEMBL4444725 Emax = 101.0 % -
CHEMBL4588694 Emax = 91.0 % -
CHEMBL559612 CP-55940 Emax = 100.0 % -
CHEMBL371214 Emax = 98.0 % -
CHEMBL497392 Emax - -