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Assay Detail

CHEMBL931641

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells
ChEMBL ↗
108
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
Frost JM, Dart MJ, Tietje KR, Garrison TR, Grayson GK, Daza AV, El-Kouhen OF, Miller LN, Li L, Yao BB, Hsieh GC, Pai M, Zhu CZ, Chandran P, Meyer MD.
J Med Chem (2008) 51 : 1904 -1912
PubMed 18311894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 108 8.18 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411631 — — 2 9.92
CHEMBL271839 — — 2 9.83
CHEMBL271158 — — 2 9.68
CHEMBL411244 — — 2 9.39
CHEMBL269851 — — 2 9.29
CHEMBL271838 — — 2 9.19
CHEMBL270125 — — 2 9.16
CHEMBL270546 — — 2 9.06
CHEMBL272868 — — 2 9.00
CHEMBL272876 — — 2 8.90
CHEMBL188 WIN-552122 — 2 8.89
CHEMBL271810 — — 2 8.86
CHEMBL409265 — — 2 8.80
CHEMBL410677 — — 2 8.80
CHEMBL270987 — — 2 8.75
CHEMBL270955 — — 2 8.72
CHEMBL411674 — — 2 8.60
CHEMBL411937 — — 2 8.54
CHEMBL271527 — — 2 8.53
CHEMBL410676 — — 2 8.52
CHEMBL271565 — — 2 8.52
CHEMBL270082 — — 2 8.50
CHEMBL408964 — — 2 8.48
CHEMBL410441 — — 2 8.46
CHEMBL259253 — — 2 8.41
CHEMBL262865 — — 2 8.36
CHEMBL272882 — — 2 8.34
CHEMBL409669 — — 2 8.31
CHEMBL410655 — — 2 8.30
CHEMBL259463 — — 2 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411631 — Ki = 0.12 nM 9.92
CHEMBL411631 — Ki = 0.1259 nM 9.90
CHEMBL271839 — Ki = 0.1479 nM 9.83
CHEMBL271839 — Ki = 0.15 nM 9.82
CHEMBL271158 — Ki = 0.21 nM 9.68
CHEMBL271158 — Ki = 0.2138 nM 9.67
CHEMBL411244 — Ki = 0.4074 nM 9.39
CHEMBL411244 — Ki = 0.41 nM 9.39
CHEMBL269851 — Ki = 0.51 nM 9.29
CHEMBL269851 — Ki = 0.5129 nM 9.29
CHEMBL271838 — Ki = 0.65 nM 9.19
CHEMBL271838 — Ki = 0.6457 nM 9.19
CHEMBL270125 — Ki = 0.6918 nM 9.16
CHEMBL270125 — Ki = 0.7 nM 9.15
CHEMBL270546 — Ki = 0.88 nM 9.06
CHEMBL270546 — Ki = 0.8913 nM 9.05
CHEMBL272868 — Ki = 1.0 nM 9.00
CHEMBL272868 — Ki = 1.023 nM 8.99
CHEMBL272876 — Ki = 1.259 nM 8.90
CHEMBL188 WIN-552122 Ki = 1.3 nM 8.89
CHEMBL188 WIN-552122 Ki = 1.288 nM 8.89
CHEMBL272876 — Ki = 1.3 nM 8.89
CHEMBL271810 — Ki = 1.38 nM 8.86
CHEMBL271810 — Ki = 1.4 nM 8.85
CHEMBL409265 — Ki = 1.585 nM 8.80
CHEMBL410677 — Ki = 1.585 nM 8.80
CHEMBL410677 — Ki = 1.6 nM 8.80
CHEMBL270987 — Ki = 1.778 nM 8.75
CHEMBL270987 — Ki = 1.8 nM 8.74
CHEMBL270955 — Ki = 1.905 nM 8.72
CHEMBL270955 — Ki = 1.9 nM 8.72
CHEMBL411674 — Ki = 2.5 nM 8.60
CHEMBL411674 — Ki = 2.512 nM 8.60
CHEMBL411937 — Ki = 2.9 nM 8.54
CHEMBL271527 — Ki = 2.951 nM 8.53
CHEMBL411937 — Ki = 2.951 nM 8.53
CHEMBL410676 — Ki = 3.0 nM 8.52
CHEMBL271527 — Ki = 3.0 nM 8.52
CHEMBL271565 — Ki = 3.02 nM 8.52
CHEMBL410676 — Ki = 3.02 nM 8.52
CHEMBL271565 — Ki = 3.1 nM 8.51
CHEMBL270082 — Ki = 3.162 nM 8.50
CHEMBL270082 — Ki = 3.2 nM 8.49
CHEMBL408964 — Ki = 3.3 nM 8.48
CHEMBL408964 — Ki = 3.311 nM 8.48
CHEMBL410441 — Ki = 3.467 nM 8.46
CHEMBL410441 — Ki = 3.5 nM 8.46
CHEMBL259253 — Ki = 3.89 nM 8.41
CHEMBL259253 — Ki = 3.9 nM 8.41
CHEMBL262865 — Ki = 4.365 nM 8.36