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Assay Detail

CHEMBL3888396

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Binding
GTPγ[35S] Functional Assay: Functional activity was evaluated using GTPγ[35S] assay in CHO membrane extracts expressing recombinant hCB1 (human CB1) receptors or hCB2 (human CB2) receptors. The assay relies on the binding of GTPγ[35S], a radiolabeled nonhydrolyzable GTP analogue, to the G protein upon binding of an agonist of the G-protein-coupled receptor. In this system, agonists stimulate GTPγ[35S] binding whereas neutral antagonist have no effect and inverse agonists decrease GTPγ[35S] basal binding.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Heterocyclic modulators of cannabinoid receptors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.05 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77520 1 8.05
CHEMBL495528 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77520 EC50 = 9.0 nM 8.05
CHEMBL495528 EC50 > 10000.0 nM -