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Assay Detail

CHEMBL4255269

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

Binding
Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB2 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method
37
Total Activities
37
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

Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
Cooper AG, MacDonald C, Glass M, Hook S, Tyndall JDA, Vernall AJ.
Eur J Med Chem (2018) 145 : 770 -789
PubMed 29407590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 6.53 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4294558 1 8.24
CHEMBL381791 1 7.29
CHEMBL4282604 1 7.27
CHEMBL4284943 1 6.92
CHEMBL78627 1 6.77
CHEMBL4283967 1 6.70
CHEMBL4293194 1 6.56
CHEMBL4279405 1 6.24
CHEMBL4277575 1 6.13
CHEMBL4292807 1 6.05
CHEMBL4291156 1 5.88
CHEMBL4287330 1 5.87
CHEMBL4295181 1 5.78
CHEMBL4294653 1 5.71
CHEMBL4282454 1 -
CHEMBL4293565 1 -
CHEMBL4282977 1 -
CHEMBL4278433 1 -
CHEMBL4286343 1 -
CHEMBL4277272 1 -
CHEMBL4291317 1 -
CHEMBL4280669 1 -
CHEMBL4281106 1 -
CHEMBL4289010 1 -
CHEMBL4284520 1 -
CHEMBL4277100 1 -
CHEMBL4286755 1 -
CHEMBL4292412 1 -
CHEMBL4278012 1 -
CHEMBL4288667 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4294558 Ki = 5.7 nM 8.24
CHEMBL381791 Ki = 51.0 nM 7.29
CHEMBL4282604 Ki = 53.9 nM 7.27
CHEMBL4284943 Ki = 120.1 nM 6.92
CHEMBL78627 Ki = 169.0 nM 6.77
CHEMBL4283967 Ki = 200.7 nM 6.70
CHEMBL4293194 Ki = 275.4 nM 6.56
CHEMBL4279405 Ki = 581.8 nM 6.24
CHEMBL4277575 Ki = 746.6 nM 6.13
CHEMBL4292807 Ki = 895.3 nM 6.05
CHEMBL4291156 Ki = 1307.0 nM 5.88
CHEMBL4287330 Ki = 1350.0 nM 5.87
CHEMBL4295181 Ki = 1660.0 nM 5.78
CHEMBL4294653 Ki = 1969.0 nM 5.71
CHEMBL4289402 Ki > 10000.0 nM -
CHEMBL4285985 Ki > 10000.0 nM -
CHEMBL4278061 Ki > 10000.0 nM -
CHEMBL4284521 Ki > 10000.0 nM -
CHEMBL4280525 Ki > 10000.0 nM -
CHEMBL4287751 Ki > 10000.0 nM -
CHEMBL4293063 Ki > 10000.0 nM -
CHEMBL4282454 Ki > 10000.0 nM -
CHEMBL4293565 Ki > 10000.0 nM -
CHEMBL4282977 Ki > 10000.0 nM -
CHEMBL4278433 Ki - -
CHEMBL4286343 Ki - -
CHEMBL4277272 Ki > 10000.0 nM -
CHEMBL4291317 Ki > 10000.0 nM -
CHEMBL4280669 Ki > 10000.0 nM -
CHEMBL4281106 Ki > 10000.0 nM -
CHEMBL4289010 Ki > 10000.0 nM -
CHEMBL4284520 Ki > 10000.0 nM -
CHEMBL4277100 Ki > 10000.0 nM -
CHEMBL4286755 Ki - -
CHEMBL4292412 Ki - -
CHEMBL4278012 Ki > 10000.0 nM -
CHEMBL4288667 Ki - -