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Assay Detail

CHEMBL820165

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Functional
In vitro antagonist activity at the vanilloid receptor in rat DRG neurons.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Vanilloid receptor (CHEMBL2096684)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.
Park HG, Choi JY, Choi SH, Park MK, Lee J, Suh YG, Cho H, Oh U, Lee J, Kang SU, Lee J, Kim HD, Park YH, Su Jeong Y, Kyu Choi J, Jew SS.
Bioorg Med Chem Lett (2004) 14 : 787 -791
PubMed 14741290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.54 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228451 1 6.96
CHEMBL164875 1 6.52
CHEMBL165272 1 6.00
CHEMBL165036 1 5.89
CHEMBL351511 1 5.82
CHEMBL167960 1 5.60
CHEMBL163834 1 5.60
CHEMBL355156 1 5.42
CHEMBL165254 1 5.39
CHEMBL434280 1 5.35
CHEMBL166987 1 5.03
CHEMBL168070 1 4.93
CHEMBL163678 1 4.91
CHEMBL164380 1 4.91
CHEMBL354812 1 4.84
CHEMBL391997 CAPSAZEPINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228451 IC50 = 110.0 nM 6.96
CHEMBL164875 IC50 = 300.0 nM 6.52
CHEMBL165272 IC50 = 1000.0 nM 6.00
CHEMBL165036 IC50 = 1300.0 nM 5.89
CHEMBL351511 IC50 = 1500.0 nM 5.82
CHEMBL167960 IC50 = 2500.0 nM 5.60
CHEMBL163834 IC50 = 2500.0 nM 5.60
CHEMBL355156 IC50 = 3800.0 nM 5.42
CHEMBL165254 IC50 = 4100.0 nM 5.39
CHEMBL434280 IC50 = 4500.0 nM 5.35
CHEMBL166987 IC50 = 9300.0 nM 5.03
CHEMBL168070 IC50 = 11700.0 nM 4.93
CHEMBL163678 IC50 = 12400.0 nM 4.91
CHEMBL164380 IC50 = 12400.0 nM 4.91
CHEMBL354812 IC50 = 14600.0 nM 4.84
CHEMBL391997 CAPSAZEPINE IC50 = 650.0 nM -