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Assay Detail

CHEMBL4668801

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

Binding
Displacement of [3H]-CP-55,940 from recombinant human CB2R expressed in HEK293 cell membranes after 90 mins
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of the Major Mammalian Metabolites of THCV.
Tinto F,Villano R,Kostrzewa M,Ligresti A,Straker H,Manzo E
J Nat Prod (2020) 83 : 2060 -2065
PubMed 32649196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.70 7.75
Ki 5 7.50 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2387541 TETRAHYDROCANNABIVARIN 2.0 2 8.55
CHEMBL4747195 2 8.33
CHEMBL4760215 2 6.89
CHEMBL4747880 2 6.23
CHEMBL4763058 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2387541 TETRAHYDROCANNABIVARIN Ki = 2.8 nM 8.55
CHEMBL4747195 Ki = 4.7 nM 8.33
CHEMBL2387541 TETRAHYDROCANNABIVARIN IC50 = 17.6 nM 7.75
CHEMBL4747195 IC50 = 29.8 nM 7.53
CHEMBL4760215 Ki = 128.2 nM 6.89
CHEMBL4747880 Ki = 589.7 nM 6.23
CHEMBL4760215 IC50 = 807.7 nM 6.09
CHEMBL4747880 IC50 = 3715.0 nM 5.43
CHEMBL4763058 IC50 > 10000.0 nM -
CHEMBL4763058 Ki > 10000.0 nM -