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Assay Detail

CHEMBL1647710

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

Binding
Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells after 1 hr
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 31 7.61 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1641956 1 9.15
CHEMBL1641955 1 8.74
CHEMBL1641945 1 8.40
CHEMBL1641943 1 8.18
CHEMBL188 WIN-552122 1 8.04
CHEMBL1641948 1 8.00
CHEMBL1641947 1 7.97
CHEMBL1641957 1 7.88
CHEMBL1641946 1 7.87
CHEMBL1641940 1 7.84
CHEMBL559612 CP-55940 1 7.81
CHEMBL1641944 1 7.74
CHEMBL1641959 1 7.73
CHEMBL1641936 1 7.70
CHEMBL1641963 1 7.69
CHEMBL1641942 1 7.63
CHEMBL1641951 1 7.59
CHEMBL1641938 1 7.54
CHEMBL1641937 1 7.54
CHEMBL1641960 1 7.32
CHEMBL1641962 1 7.29
CHEMBL381689 SR-144528 1 7.29
CHEMBL1641953 1 7.11
CHEMBL1641952 1 7.10
CHEMBL1641950 1 7.04
CHEMBL1641958 1 7.04
CHEMBL1641961 1 6.68
CHEMBL1641949 1 6.43
CHEMBL1641939 1 6.38
CHEMBL1641954 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1641956 Ki = 0.7 nM 9.15
CHEMBL1641955 Ki = 1.8 nM 8.74
CHEMBL1641945 Ki = 4.0 nM 8.40
CHEMBL1641943 Ki = 6.6 nM 8.18
CHEMBL188 WIN-552122 Ki = 9.1 nM 8.04
CHEMBL1641948 Ki = 10.1 nM 8.00
CHEMBL1641947 Ki = 10.6 nM 7.97
CHEMBL1641957 Ki = 13.2 nM 7.88
CHEMBL1641946 Ki = 13.5 nM 7.87
CHEMBL1641940 Ki = 14.3 nM 7.84
CHEMBL559612 CP-55940 Ki = 15.4 nM 7.81
CHEMBL1641944 Ki = 18.4 nM 7.74
CHEMBL1641959 Ki = 18.8 nM 7.73
CHEMBL1641936 Ki = 20.0 nM 7.70
CHEMBL1641963 Ki = 20.3 nM 7.69
CHEMBL1641942 Ki = 23.3 nM 7.63
CHEMBL1641951 Ki = 25.8 nM 7.59
CHEMBL1641938 Ki = 29.0 nM 7.54
CHEMBL1641937 Ki = 29.0 nM 7.54
CHEMBL1641960 Ki = 48.0 nM 7.32
CHEMBL1641962 Ki = 51.0 nM 7.29
CHEMBL381689 SR-144528 Ki = 51.7 nM 7.29
CHEMBL1641953 Ki = 78.0 nM 7.11
CHEMBL1641952 Ki = 79.0 nM 7.10
CHEMBL1641950 Ki = 92.0 nM 7.04
CHEMBL1641958 Ki = 91.1 nM 7.04
CHEMBL1641961 Ki = 209.0 nM 6.68
CHEMBL1641949 Ki = 369.0 nM 6.43
CHEMBL1641939 Ki = 414.0 nM 6.38
CHEMBL1641954 Ki > 1000.0 nM -
CHEMBL1641941 Ki > 3000.0 nM -