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Assay Detail

CHEMBL3862618

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

Binding
Antagonist activity at rat TRPV3 overexpressed in HEK293 cells assessed as inhibition of thymol-induced increase in intracellular Ca2+ levels preincubated for 5 mins prior to thymol-stimulation by Fluo-4AM dye-based spectrofluorometry
14
Total Activities
14
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 Autocuration

Target

Heat sensitive channel TRPV3 (CHEMBL3879847)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Neuroactive and Anti-inflammatory Frankincense Cembranes: A Structure-Activity Study.
Pollastro F, Golin S, Chianese G, Putra MY, Schiano Moriello A, De Petrocellis L, García V, Munoz E, Taglialatela-Scafati O, Appendino G.
J Nat Prod (2016) 79 : 1762 -1768
PubMed 27352042 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.04 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3943485 1 6.82
CHEMBL497044 INCENSOLE 1 5.68
CHEMBL3979367 1 5.66
CHEMBL3983336 1 5.24
CHEMBL3922508 1 4.91
CHEMBL3975348 1 4.88
CHEMBL3913521 1 4.68
CHEMBL3890789 1 4.66
CHEMBL3899770 1 4.62
CHEMBL3894504 1 4.24
CHEMBL3948101 1 4.03
CHEMBL3959869 1 -
CHEMBL3904515 1 -
CHEMBL3931428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3943485 IC50 = 150.0 nM 6.82
CHEMBL497044 INCENSOLE IC50 = 2100.0 nM 5.68
CHEMBL3979367 IC50 = 2200.0 nM 5.66
CHEMBL3983336 IC50 = 5800.0 nM 5.24
CHEMBL3922508 IC50 = 12300.0 nM 4.91
CHEMBL3975348 IC50 = 13200.0 nM 4.88
CHEMBL3913521 IC50 = 21100.0 nM 4.68
CHEMBL3890789 IC50 = 21700.0 nM 4.66
CHEMBL3899770 IC50 = 24100.0 nM 4.62
CHEMBL3894504 IC50 = 57500.0 nM 4.24
CHEMBL3948101 IC50 = 94400.0 nM 4.03
CHEMBL3959869 IC50 > 100000.0 nM -
CHEMBL3904515 IC50 > 100000.0 nM -
CHEMBL3931428 IC50 > 100000.0 nM -