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Assay Detail

CHEMBL828244

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

Binding
Inhibition of human transient receptor potential vanilloid 1 receptor (n=5)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Publication

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI.
J Med Chem (2005) 48 : 1857 -1872
PubMed 15771431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.66 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391997 CAPSAZEPINE 1 7.13
CHEMBL3138733 1 6.58
CHEMBL367039 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391997 CAPSAZEPINE IC50 = 74.0 nM 7.13
CHEMBL3138733 IC50 = 260.0 nM 6.58
CHEMBL367039 IC50 = 526.0 nM 6.28