Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1006420

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

Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
Cheng Y, Albrecht BK, Brown J, Buchanan JL, Buckner WH, DiMauro EF, Emkey R, Fremeau RT, Harmange JC, Hoffman BJ, Huang L, Huang M, Lee JH, Lin FF, Martin MW, Nguyen HQ, Patel VF, Tomlinson SA, White RD, Xia X, Hitchcock SA.
J Med Chem (2008) 51 : 5019 -5034
PubMed 18680277 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 41 6.62 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 9.59
CHEMBL499628 1 6.48
CHEMBL499065 1 6.25
CHEMBL526345 1 6.15
CHEMBL499066 1 6.07
CHEMBL498469 1 6.00
CHEMBL524826 1 5.82
CHEMBL499331 1 -
CHEMBL500670 1 -
CHEMBL498324 1 -
CHEMBL498323 1 -
CHEMBL498322 1 -
CHEMBL540704 1 -
CHEMBL500927 1 -
CHEMBL498470 1 -
CHEMBL526471 1 -
CHEMBL525019 1 -
CHEMBL498795 1 -
CHEMBL453993 1 -
CHEMBL527051 1 -
CHEMBL499328 1 -
CHEMBL499877 1 -
CHEMBL499626 1 -
CHEMBL526322 1 -
CHEMBL499627 1 -
CHEMBL527095 1 -
CHEMBL501472 1 -
CHEMBL499324 1 -
CHEMBL499601 1 -
CHEMBL499332 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 EC50 = 0.26 nM 9.59
CHEMBL499628 EC50 = 330.0 nM 6.48
CHEMBL499065 EC50 = 560.0 nM 6.25
CHEMBL526345 EC50 = 710.0 nM 6.15
CHEMBL499066 EC50 = 850.0 nM 6.07
CHEMBL498469 EC50 = 990.0 nM 6.00
CHEMBL524826 EC50 = 1500.0 nM 5.82
CHEMBL500927 EC50 > 1000.0 nM -
CHEMBL499050 EC50 > 1000.0 nM -
CHEMBL498470 EC50 > 1000.0 nM -
CHEMBL526471 EC50 - -
CHEMBL525019 EC50 > 1000.0 nM -
CHEMBL498795 EC50 > 1000.0 nM -
CHEMBL500670 EC50 > 1000.0 nM -
CHEMBL524839 EC50 > 1000.0 nM -
CHEMBL499060 EC50 > 1000.0 nM -
CHEMBL499059 EC50 > 1000.0 nM -
CHEMBL500655 EC50 > 1000.0 nM -
CHEMBL500926 EC50 > 1000.0 nM -
CHEMBL524680 EC50 > 1000.0 nM -
CHEMBL500134 EC50 - -
CHEMBL500133 EC50 > 1000.0 nM -
CHEMBL499874 EC50 - -
CHEMBL502263 EC50 > 1000.0 nM -
CHEMBL499877 EC50 - -
CHEMBL499332 EC50 > 1000.0 nM -
CHEMBL499601 EC50 > 1000.0 nM -
CHEMBL499324 EC50 > 1000.0 nM -
CHEMBL501472 EC50 > 1000.0 nM -
CHEMBL527095 EC50 > 1000.0 nM -
CHEMBL499627 EC50 - -
CHEMBL526322 EC50 - -
CHEMBL499626 EC50 - -
CHEMBL540704 EC50 > 1000.0 nM -
CHEMBL499328 EC50 > 1000.0 nM -
CHEMBL527051 EC50 - -
CHEMBL453993 EC50 - -
CHEMBL499331 EC50 - -
CHEMBL498324 EC50 - -
CHEMBL498323 EC50 - -
CHEMBL498322 EC50 - -