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Assay Detail

CHEMBL834034

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Functional
Agonist activity by [Ca2+] uptake in CHO cells expressing rat TRPV1 at 10-30 uM
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Publication

Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Lee J, Kang SU, Kil MJ, Shin M, Lim JO, Choi HK, Jin MK, Kim SY, Kim SE, Lee YS, Min KH, Kim YH, Ha HJ, Tran R, Welter JD, Wang Y, Szabo T, Pearce LV, Lundberg DJ, Toth A, Pavlyukovets VA, Morgan MA, Blumberg PM.
Bioorg Med Chem Lett (2005) 15 : 4136 -4142
PubMed 16005215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.18 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426266 1 6.60
CHEMBL188264 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426266 EC50 = 250.0 nM 6.60
CHEMBL188264 EC50 = 1720.0 nM 5.76