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Assay Detail

CHEMBL1068424

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Functional
Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level
9
Total Activities
9
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 Autocuration

Publication

Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): The side chain benzylic methylene.
Appendino G, Ech-Chahad A, Minassi A, De Petrocellis L, Di Marzo V.
Bioorg Med Chem Lett (2010) 20 : 97 -99
PubMed 19951840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.69 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17976 RESINIFERATOXIN 3.0 1 10.72
CHEMBL594016 1 9.82
CHEMBL594649 1 9.19
CHEMBL594895 1 9.01
CHEMBL593623 1 7.86
CHEMBL594862 1 7.76
CHEMBL595046 1 7.72
CHEMBL294199 CAPSAICIN 4.0 1 7.40
CHEMBL595262 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17976 RESINIFERATOXIN EC50 = 0.019 nM 10.72
CHEMBL594016 EC50 = 0.15 nM 9.82
CHEMBL594649 EC50 = 0.65 nM 9.19
CHEMBL594895 EC50 = 0.98 nM 9.01
CHEMBL593623 EC50 = 13.7 nM 7.86
CHEMBL594862 EC50 = 17.4 nM 7.76
CHEMBL595046 EC50 = 19.0 nM 7.72
CHEMBL294199 CAPSAICIN EC50 = 40.0 nM 7.40
CHEMBL595262 EC50 = 0.0047 nM -