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Assay Detail

CHEMBL900693

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Binding
Inhibition of human CB2 receptor expressed in CHO cells
ChEMBL ↗
65
Total Activities
57
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 Intermediate

Target

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

Publication

Pharmacomodulations around the 4-oxo-1,4-dihydroquinoline-3-carboxamides, a class of potent CB2-selective cannabinoid receptor ligands: consequences in receptor affinity and functionality.
Stern E, Muccioli GG, Bosier B, Hamtiaux L, Millet R, Poupaert JH, Hénichart JP, Depreux P, Goossens JF, Lambert DM.
J Med Chem (2007) 50 : 5471 -5484
PubMed 17915849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 65 6.76 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235733 — — 1 8.28
CHEMBL236333 — — 3 7.85
CHEMBL236361 — — 1 7.74
CHEMBL235040 — — 1 7.63
CHEMBL393792 — — 1 7.59
CHEMBL237010 — — 3 7.58
CHEMBL235946 — — 1 7.56
CHEMBL392288 — — 1 7.51
CHEMBL380610 — — 2 7.38
CHEMBL235487 — — 1 7.30
CHEMBL235732 — — 1 7.26
CHEMBL238047 — — 1 7.08
CHEMBL235042 — — 1 7.03
CHEMBL235335 — — 2 6.92
CHEMBL393931 — — 1 6.92
CHEMBL235947 — — 3 6.84
CHEMBL392952 — — 1 6.82
CHEMBL235908 — — 1 6.81
CHEMBL394230 — — 1 6.80
CHEMBL236539 — — 1 6.70
CHEMBL235900 — — 1 6.66
CHEMBL235278 — — 1 6.65
CHEMBL429986 — — 1 6.59
CHEMBL428553 — — 1 6.58
CHEMBL238048 — — 1 6.48
CHEMBL237171 — — 1 6.47
CHEMBL237166 — — 1 6.35
CHEMBL235057 — — 1 6.24
CHEMBL393615 — — 1 6.18
CHEMBL236551 — — 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235733 — Ki = 5.3 nM 8.28
CHEMBL236333 — Ki = 14.0 nM 7.85
CHEMBL236361 — Ki = 18.2 nM 7.74
CHEMBL235040 — Ki = 23.5 nM 7.63
CHEMBL393792 — Ki = 25.5 nM 7.59
CHEMBL237010 — Ki = 26.1 nM 7.58
CHEMBL235946 — Ki = 27.4 nM 7.56
CHEMBL236333 — Ki = 28.5 nM 7.54
CHEMBL392288 — Ki = 30.9 nM 7.51
CHEMBL237010 — Ki = 41.1 nM 7.39
CHEMBL380610 — Ki = 41.7 nM 7.38
CHEMBL235487 — Ki = 50.6 nM 7.30
CHEMBL235732 — Ki = 54.6 nM 7.26
CHEMBL238047 — Ki = 83.4 nM 7.08
CHEMBL235042 — Ki = 93.0 nM 7.03
CHEMBL393931 — Ki = 119.0 nM 6.92
CHEMBL235335 — Ki = 121.0 nM 6.92
CHEMBL235947 — Ki = 144.0 nM 6.84
CHEMBL392952 — Ki = 152.0 nM 6.82
CHEMBL235908 — Ki = 154.0 nM 6.81
CHEMBL394230 — Ki = 160.0 nM 6.80
CHEMBL236333 — Ki = 202.0 nM 6.70
CHEMBL236539 — Ki = 200.0 nM 6.70
CHEMBL235900 — Ki = 221.0 nM 6.66
CHEMBL235278 — Ki = 225.0 nM 6.65
CHEMBL235947 — Ki = 222.0 nM 6.65
CHEMBL235947 — Ki = 235.0 nM 6.63
CHEMBL429986 — Ki = 259.0 nM 6.59
CHEMBL237010 — Ki = 265.0 nM 6.58
CHEMBL428553 — Ki = 265.0 nM 6.58
CHEMBL238048 — Ki = 333.0 nM 6.48
CHEMBL237171 — Ki = 338.0 nM 6.47
CHEMBL237166 — Ki = 446.0 nM 6.35
CHEMBL235335 — Ki = 506.0 nM 6.30
CHEMBL235057 — Ki = 582.0 nM 6.24
CHEMBL236551 — Ki = 663.0 nM 6.18
CHEMBL393615 — Ki = 656.0 nM 6.18
CHEMBL236548 — Ki = 966.0 nM 6.01
CHEMBL380610 — Ki = 1010.0 nM 6.00
CHEMBL394140 — Ki = 1120.0 nM 5.95
CHEMBL397762 — Ki = 1130.0 nM 5.95
CHEMBL236961 — Ki = 1288.0 nM 5.89
CHEMBL236972 — Ki = 1500.0 nM 5.82
CHEMBL235698 — Ki = 1550.0 nM 5.81
CHEMBL236156 — Ki = 1670.0 nM 5.78
CHEMBL236962 — Ki = 1670.0 nM 5.78
CHEMBL237167 — Ki - — -
CHEMBL236753 — Ki - — -
CHEMBL392138 — Ki - — -
CHEMBL401426 — Ki - — -