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Assay Detail

CHEMBL4255281

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

Functional
Agonist activity at N-terminal HA-tagged human CB1 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as decrease in forskolin-stimulated cAMP level by BRET assay
12
Total Activities
12
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

Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
Cooper AG, MacDonald C, Glass M, Hook S, Tyndall JDA, Vernall AJ.
Eur J Med Chem (2018) 145 : 770 -789
PubMed 29407590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.70 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4284943 1 7.20
CHEMBL4282604 1 6.20
CHEMBL4277575 1 -
CHEMBL78627 1 -
CHEMBL4292807 1 -
CHEMBL4293194 1 -
CHEMBL4295181 1 -
CHEMBL4279405 1 -
CHEMBL4283967 1 -
CHEMBL4291156 1 -
CHEMBL4294653 1 -
CHEMBL559612 CP-55940 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4284943 EC50 = 62.9 nM 7.20
CHEMBL4282604 EC50 = 632.5 nM 6.20
CHEMBL4277575 EC50 - -
CHEMBL78627 EC50 - -
CHEMBL4292807 EC50 - -
CHEMBL4293194 EC50 - -
CHEMBL4295181 EC50 - -
CHEMBL4279405 EC50 - -
CHEMBL4283967 EC50 - -
CHEMBL4291156 EC50 - -
CHEMBL4294653 EC50 - -
CHEMBL559612 CP-55940 EC50 - -