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Assay Detail

CHEMBL833627

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Functional
Agonist activity by [Ca2+] uptake in CHO cells expressing rat TRPV1 at 10-30 uM; NE = Not effective
15
Total Activities
15
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 15 5.56 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424803 1 5.72
CHEMBL189507 1 5.39
CHEMBL391997 CAPSAZEPINE 1 -
CHEMBL228451 1 -
CHEMBL388824 1 -
CHEMBL189418 1 -
CHEMBL189177 1 -
CHEMBL191024 1 -
CHEMBL363267 1 -
CHEMBL190637 1 -
CHEMBL365213 1 -
CHEMBL370055 1 -
CHEMBL425180 1 -
CHEMBL187838 1 -
CHEMBL370264 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424803 EC50 = 1890.0 nM 5.72
CHEMBL189507 EC50 = 4100.0 nM 5.39
CHEMBL391997 CAPSAZEPINE EC50 - nM -
CHEMBL228451 EC50 - nM -
CHEMBL388824 EC50 - nM -
CHEMBL189418 EC50 - nM -
CHEMBL189177 EC50 - nM -
CHEMBL191024 EC50 - nM -
CHEMBL363267 EC50 - nM -
CHEMBL190637 EC50 - nM -
CHEMBL365213 EC50 - nM -
CHEMBL370055 EC50 - nM -
CHEMBL425180 EC50 - nM -
CHEMBL187838 EC50 - nM -
CHEMBL370264 EC50 - nM -