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Assay Detail

CHEMBL4235230

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

Binding
Antagonist activity at rat TRPV3 expressed in HEK293 cells assessed as inhibition of thymol-induced increase in intracellular calcium level pretreated for 5 mins followed by thymol addition by Fluo-4-AM dye based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Publication

Iodine-mediated cyclization of cannabigerol (CBG) expands the cannabinoid biological and chemical space.
Lopatriello A, Caprioglio D, Minassi A, Schiano Moriello A, Formisano C, De Petrocellis L, Appendino G, Taglialatela-Scafati O.
Bioorg Med Chem (2018) 26 : 4532 -4536
PubMed 30077611 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.00 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4249046 1 5.10
CHEMBL4238545 1 4.89
CHEMBL4244422 1 -
CHEMBL4238978 1 -
CHEMBL4242719 1 -
CHEMBL4241477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4249046 IC50 = 8000.0 nM 5.10
CHEMBL4238545 IC50 = 12800.0 nM 4.89
CHEMBL4244422 IC50 > 50000.0 nM -
CHEMBL4238978 IC50 > 50000.0 nM -
CHEMBL4242719 IC50 > 50000.0 nM -
CHEMBL4241477 IC50 > 50000.0 nM -