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Assay Detail

CHEMBL2183177

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 incubated for 1 hr
ChEMBL ↗
94
Total Activities
54
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

Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors.
Yang P, Myint KZ, Tong Q, Feng R, Cao H, Almehizia AA, Alqarni MH, Wang L, Bartlow P, Gao Y, Gertsch J, Teramachi J, Kurihara N, Roodman GD, Cheng T, Xie XQ.
J Med Chem (2012) 55 : 9973 -9987
PubMed 23072339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 94 6.09 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381689 SR-144528 — 1 8.68
CHEMBL2179751 — — 2 7.66
CHEMBL2179734 — — 2 7.60
CHEMBL2179771 — — 2 7.19
CHEMBL2179754 — — 2 7.15
CHEMBL2179763 — — 2 7.07
CHEMBL2179740 — — 2 7.00
CHEMBL2179735 — — 2 6.84
CHEMBL2179759 — — 2 6.81
CHEMBL2179739 — — 2 6.80
CHEMBL2179736 — — 2 6.80
CHEMBL2179728 — — 2 6.78
CHEMBL2179733 — — 2 6.74
CHEMBL2179753 — — 2 6.69
CHEMBL2179727 — — 2 6.67
CHEMBL2179752 — — 2 6.66
CHEMBL2179738 — — 2 6.51
CHEMBL2179766 — — 2 6.50
CHEMBL2179737 — — 2 6.33
CHEMBL2179762 — — 2 6.31
CHEMBL2179768 — — 2 6.22
CHEMBL2179755 — — 2 6.22
CHEMBL2179726 — — 2 6.16
CHEMBL2179776 — — 2 6.11
CHEMBL2179764 — — 2 6.11
CHEMBL2179765 — — 2 5.82
CHEMBL2179761 — — 2 5.65
CHEMBL2179731 — — 2 5.58
CHEMBL2179760 — — 2 5.51
CHEMBL2179732 — — 2 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381689 SR-144528 Ki = 2.1 nM 8.68
CHEMBL2179751 — Ki = 22.0 nM 7.66
CHEMBL2179751 — Ki = 22.0 nM 7.66
CHEMBL2179734 — Ki = 25.0 nM 7.60
CHEMBL2179734 — Ki = 25.0 nM 7.60
CHEMBL2179771 — Ki = 64.0 nM 7.19
CHEMBL2179771 — Ki = 64.0 nM 7.19
CHEMBL2179754 — Ki = 71.0 nM 7.15
CHEMBL2179754 — Ki = 71.0 nM 7.15
CHEMBL2179763 — Ki = 85.0 nM 7.07
CHEMBL2179763 — Ki = 85.0 nM 7.07
CHEMBL2179740 — Ki = 101.0 nM 7.00
CHEMBL2179740 — Ki = 101.0 nM 7.00
CHEMBL2179735 — Ki = 146.0 nM 6.84
CHEMBL2179735 — Ki = 146.0 nM 6.84
CHEMBL2179759 — Ki = 154.0 nM 6.81
CHEMBL2179759 — Ki = 154.0 nM 6.81
CHEMBL2179739 — Ki = 158.0 nM 6.80
CHEMBL2179739 — Ki = 158.0 nM 6.80
CHEMBL2179736 — Ki = 160.0 nM 6.80
CHEMBL2179736 — Ki = 160.0 nM 6.80
CHEMBL2179728 — Ki = 167.0 nM 6.78
CHEMBL2179728 — Ki = 167.0 nM 6.78
CHEMBL2179733 — Ki = 182.0 nM 6.74
CHEMBL2179733 — Ki = 182.0 nM 6.74
CHEMBL2179753 — Ki = 203.0 nM 6.69
CHEMBL2179753 — Ki = 203.0 nM 6.69
CHEMBL2179727 — Ki = 213.0 nM 6.67
CHEMBL2179727 — Ki = 213.0 nM 6.67
CHEMBL2179752 — Ki = 221.0 nM 6.66
CHEMBL2179752 — Ki = 221.0 nM 6.66
CHEMBL2179738 — Ki = 310.0 nM 6.51
CHEMBL2179738 — Ki = 310.0 nM 6.51
CHEMBL2179766 — Ki = 313.0 nM 6.50
CHEMBL2179766 — Ki = 313.0 nM 6.50
CHEMBL2179737 — Ki = 462.0 nM 6.33
CHEMBL2179737 — Ki = 462.0 nM 6.33
CHEMBL2179762 — Ki = 494.0 nM 6.31
CHEMBL2179762 — Ki = 494.0 nM 6.31
CHEMBL2179755 — Ki = 595.0 nM 6.22
CHEMBL2179768 — Ki = 596.0 nM 6.22
CHEMBL2179755 — Ki = 595.0 nM 6.22
CHEMBL2179768 — Ki = 596.0 nM 6.22
CHEMBL2179726 — Ki = 688.0 nM 6.16
CHEMBL2179726 — Ki = 688.0 nM 6.16
CHEMBL2179764 — Ki = 783.0 nM 6.11
CHEMBL2179776 — Ki = 777.0 nM 6.11
CHEMBL2179764 — Ki = 783.0 nM 6.11
CHEMBL2179776 — Ki = 777.0 nM 6.11
CHEMBL2179765 — Ki = 1500.0 nM 5.82