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Assay Detail

CHEMBL1647712

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Functional
Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.
El Bakali J, Muccioli GG, Renault N, Pradal D, Body-Malapel M, Djouina M, Hamtiaux L, Andrzejak V, Desreumaux P, Chavatte P, Lambert DM, Millet R.
J Med Chem (2010) 53 : 7918 -7931
PubMed 20979417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 7.87 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381689 SR-144528 1 8.74
CHEMBL1641948 1 8.72
CHEMBL1641947 1 8.72
CHEMBL1641945 1 8.49
CHEMBL1641936 1 8.26
CHEMBL1641943 1 8.24
CHEMBL559612 CP-55940 1 8.21
CHEMBL1641940 1 8.19
CHEMBL1641944 1 8.13
CHEMBL1641938 1 8.11
CHEMBL1641946 1 8.06
CHEMBL1641942 1 7.96
CHEMBL1641937 1 7.91
CHEMBL1641951 1 7.85
CHEMBL1641959 1 7.77
CHEMBL1641953 1 7.66
CHEMBL1641952 1 7.64
CHEMBL188 WIN-552122 1 7.61
CHEMBL1641962 1 7.60
CHEMBL1641950 1 7.58
CHEMBL1641960 1 7.57
CHEMBL1641949 1 7.22
CHEMBL1641963 1 6.84
CHEMBL1641954 1 6.80
CHEMBL1641961 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381689 SR-144528 EC50 = 1.8 nM 8.74
CHEMBL1641948 EC50 = 1.9 nM 8.72
CHEMBL1641947 EC50 = 1.9 nM 8.72
CHEMBL1641945 EC50 = 3.2 nM 8.49
CHEMBL1641936 EC50 = 5.5 nM 8.26
CHEMBL1641943 EC50 = 5.8 nM 8.24
CHEMBL559612 CP-55940 EC50 = 6.1 nM 8.21
CHEMBL1641940 EC50 = 6.5 nM 8.19
CHEMBL1641944 EC50 = 7.4 nM 8.13
CHEMBL1641938 EC50 = 7.8 nM 8.11
CHEMBL1641946 EC50 = 8.7 nM 8.06
CHEMBL1641942 EC50 = 10.9 nM 7.96
CHEMBL1641937 EC50 = 12.2 nM 7.91
CHEMBL1641951 EC50 = 14.0 nM 7.85
CHEMBL1641959 EC50 = 17.0 nM 7.77
CHEMBL1641953 EC50 = 22.0 nM 7.66
CHEMBL1641952 EC50 = 23.0 nM 7.64
CHEMBL188 WIN-552122 EC50 = 24.6 nM 7.61
CHEMBL1641962 EC50 = 25.0 nM 7.60
CHEMBL1641950 EC50 = 26.0 nM 7.58
CHEMBL1641960 EC50 = 27.0 nM 7.57
CHEMBL1641949 EC50 = 60.0 nM 7.22
CHEMBL1641963 EC50 = 145.6 nM 6.84
CHEMBL1641954 EC50 = 158.0 nM 6.80
CHEMBL1641961 EC50 = 164.0 nM 6.79