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Assay Detail

CHEMBL4023567

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

Binding
Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method
ChEMBL ↗
37
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles.
Dolles D, Hoffmann M, Gunesch S, Marinelli O, Möller J, Santoni G, Chatonnet A, Lohse MJ, Wittmann HJ, Strasser A, Nabissi M, Maurice T, Decker M.
J Med Chem (2018) 61 : 1646 -1663
PubMed 29400965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.90 7.71
IC50 18 5.88 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381791 — — 2 7.71
CHEMBL471980 — — 2 7.43
CHEMBL4082936 — — 2 6.73
CHEMBL4075256 — — 2 6.45
CHEMBL4104311 — — 2 6.42
CHEMBL4100917 — — 2 6.37
CHEMBL4061358 — — 2 6.12
CHEMBL4104374 — — 2 6.02
CHEMBL4082785 — — 2 6.00
CHEMBL4086412 — — 2 5.72
CHEMBL4079520 — — 2 5.72
CHEMBL4099175 — — 2 5.40
CHEMBL4063907 — — 2 5.33
CHEMBL4085482 — — 2 5.32
CHEMBL4074747 — — 2 5.10
CHEMBL4095946 — — 2 4.98
CHEMBL4076334 — — 2 4.84
CHEMBL4070526 — — 2 4.70
CHEMBL95 TACRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381791 — Ki = 19.7 nM 7.71
CHEMBL381791 — IC50 = 19.95 nM 7.70
CHEMBL471980 — Ki = 36.7 nM 7.43
CHEMBL471980 — IC50 = 39.81 nM 7.40
CHEMBL4082936 — Ki = 188.0 nM 6.73
CHEMBL4082936 — IC50 = 199.53 nM 6.70
CHEMBL4075256 — Ki = 353.4 nM 6.45
CHEMBL4104311 — Ki = 384.5 nM 6.42
CHEMBL4075256 — IC50 = 398.11 nM 6.40
CHEMBL4104311 — IC50 = 398.11 nM 6.40
CHEMBL4100917 — Ki = 426.0 nM 6.37
CHEMBL4100917 — IC50 = 501.19 nM 6.30
CHEMBL4061358 — Ki = 763.6 nM 6.12
CHEMBL4061358 — IC50 = 794.33 nM 6.10
CHEMBL4104374 — Ki = 961.8 nM 6.02
CHEMBL4082785 — Ki = 1000.0 nM 6.00
CHEMBL4104374 — IC50 = 1000.0 nM 6.00
CHEMBL4082785 — IC50 = 1258.93 nM 5.90
CHEMBL4086412 — Ki = 1900.0 nM 5.72
CHEMBL4079520 — Ki = 1900.0 nM 5.72
CHEMBL4079520 — IC50 = 1995.26 nM 5.70
CHEMBL4086412 — IC50 = 1995.26 nM 5.70
CHEMBL4099175 — IC50 = 3981.07 nM 5.40
CHEMBL4099175 — Ki = 4300.0 nM 5.37
CHEMBL4063907 — Ki = 4700.0 nM 5.33
CHEMBL4085482 — Ki = 4800.0 nM 5.32
CHEMBL4063907 — IC50 = 5011.87 nM 5.30
CHEMBL4085482 — IC50 = 5011.87 nM 5.30
CHEMBL4074747 — IC50 = 7943.28 nM 5.10
CHEMBL4074747 — Ki = 8900.0 nM 5.05
CHEMBL4095946 — Ki = 10400.0 nM 4.98
CHEMBL4095946 — IC50 = 12589.25 nM 4.90
CHEMBL4076334 — Ki = 14400.0 nM 4.84
CHEMBL4076334 — IC50 = 15848.93 nM 4.80
CHEMBL4070526 — IC50 = 19952.62 nM 4.70
CHEMBL4070526 — Ki = 21000.0 nM 4.68
CHEMBL95 TACRINE Ki - — -