Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5055756

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

Functional
Antinociceptive activity against AITC-induced rat pain model assessed as nocifensive behaviour by measuring unbound concentration
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Autocuration

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.
Terrett JA, Chen H, Shore DG, Villemure E, Larouche-Gauthier R, Déry M, Beaumier F, Constantineau-Forget L, Grand-Maître C, Lépissier L, Ciblat S, Sturino C, Chen Y, Hu B, Lu A, Wang Y, Cridland AP, Ward SI, Hackos DH, Reese RM, Shields SD, Chen J, Balestrini A, Riol-Blanco L, Lee WP, Liu J, Suto E, Wu X, Zhang J, Ly JQ, La H, Johnson K, Baumgardner M, Chou KJ, Rohou A, Rougé L, Safina BS, Magnuson S, Volgraf M.
J Med Chem (2021) 64 : 3843 -3869
PubMed 33749283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.33 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5094919 1 8.21
CHEMBL4870870 1 8.10
CHEMBL5093753 1 7.31
CHEMBL4849329 1 7.28
CHEMBL5091060 1 6.66
CHEMBL4863686 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5094919 EC50 = 6.2 nM 8.21
CHEMBL4870870 EC50 = 7.9 nM 8.10
CHEMBL5093753 EC50 = 49.0 nM 7.31
CHEMBL4849329 EC50 = 53.0 nM 7.28
CHEMBL5091060 EC50 = 220.0 nM 6.66
CHEMBL4863686 EC50 = 390.0 nM 6.41