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Assay Detail

CHEMBL889822

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Functional
Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Publication

Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety.
Appendino G, Ech-Chahad A, Minassi A, Bacchiega S, De Petrocellis L, Di Marzo V.
Bioorg Med Chem Lett (2007) 17 : 132 -135
PubMed 17046253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.18 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17976 RESINIFERATOXIN 3.0 1 10.72
CHEMBL234520 1 8.82
CHEMBL438313 1 8.72
CHEMBL391598 1 8.34
CHEMBL391808 1 8.33
CHEMBL233915 1 8.10
CHEMBL232947 1 8.07
CHEMBL391393 1 8.03
CHEMBL438140 1 7.82
CHEMBL391807 1 7.59
CHEMBL294199 CAPSAICIN 4.0 1 7.40
CHEMBL234752 1 7.29
CHEMBL392462 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17976 RESINIFERATOXIN EC50 = 0.019 nM 10.72
CHEMBL234520 EC50 = 1.5 nM 8.82
CHEMBL438313 EC50 = 1.9 nM 8.72
CHEMBL391598 EC50 = 4.6 nM 8.34
CHEMBL391808 EC50 = 4.7 nM 8.33
CHEMBL233915 EC50 = 7.9 nM 8.10
CHEMBL232947 EC50 = 8.6 nM 8.07
CHEMBL391393 EC50 = 9.4 nM 8.03
CHEMBL438140 EC50 = 15.2 nM 7.82
CHEMBL391807 EC50 = 25.5 nM 7.59
CHEMBL294199 CAPSAICIN EC50 = 40.0 nM 7.40
CHEMBL234752 EC50 = 51.5 nM 7.29
CHEMBL392462 EC50 = 69.5 nM 7.16