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Assay Detail

CHEMBL998520

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Functional
Agonist-enhancing activity in epsilon-epitope tagged TRPV1 receptor expressed in mouse NIH3T3 cells assessed as capsaicin-induced 45Ca2+ influx by microplate liquid scintillation counter
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Intermediate

Publication

Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
Roh EJ, Keller JM, Olah Z, Iadarola MJ, Jacobson KA.
Bioorg Med Chem (2008) 16 : 9349 -9358
PubMed 18809334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 4.58 4.77
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485726 1 4.77
CHEMBL109081 1 4.67
CHEMBL470161 1 4.66
CHEMBL323042 1 4.65
CHEMBL505916 1 4.57
CHEMBL469757 1 4.56
CHEMBL511970 1 4.55
CHEMBL108801 1 4.55
CHEMBL485925 1 4.54
CHEMBL472235 1 4.29
CHEMBL1484 NICARDIPINE 4.0 1 -
CHEMBL283013 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485726 EC50 = 17100.0 nM 4.77
CHEMBL109081 EC50 = 21300.0 nM 4.67
CHEMBL470161 EC50 = 21800.0 nM 4.66
CHEMBL323042 EC50 = 22400.0 nM 4.65
CHEMBL505916 EC50 = 26700.0 nM 4.57
CHEMBL469757 EC50 = 27600.0 nM 4.56
CHEMBL511970 EC50 = 28400.0 nM 4.55
CHEMBL108801 EC50 = 28100.0 nM 4.55
CHEMBL485925 EC50 = 29200.0 nM 4.54
CHEMBL472235 EC50 = 51600.0 nM 4.29
CHEMBL1484 NICARDIPINE Activity - -
CHEMBL283013 Activity - -