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Assay Detail

CHEMBL4734809

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

Binding
Agonist activity at TRPV1 in rat isolated mesenteric arteries assessed as vasorelaxation of phenylephrine-induced contraction in presence of TRPV1 antagonist capsazepine
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Artery
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Paracetamol analogues conjugated by FAAH induce TRPV1-mediated antinociception without causing acute liver toxicity.
Å Nilsson JL,Mallet C,Shionoya K,Blomgren A,Sundin AP,Grundemar L,Boudieu L,Blomqvist A,Eschalier A,Nilsson UJ,Zygmunt PM
Eur J Med Chem (2021) 213 : 113042 -113042
PubMed 33257173 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.05 7.80
pEC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL472898 1 7.80
CHEMBL4747170 1 7.20
CHEMBL4778235 1 6.80
CHEMBL472897 1 6.40
CHEMBL39878 1 -
CHEMBL123254 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL472898 EC50 = 15.85 nM 7.80
CHEMBL4747170 EC50 = 63.1 nM 7.20
CHEMBL4778235 EC50 = 158.49 nM 6.80
CHEMBL472897 EC50 = 398.11 nM 6.40
CHEMBL39878 pEC50 - -
CHEMBL123254 pEC50 - -