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Assay Detail

CHEMBL3888397

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Functional
cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Heterocyclic modulators of cannabinoid receptors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 9.85 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77520 1 9.85
CHEMBL495528 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77520 EC50 = 0.14 nM 9.85
CHEMBL495528 EC50 > 10000.0 nM -