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Assay Detail

CHEMBL779560

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
In vitro inhibitory concentration was determined against [45Ca2+]- influx in rat DRG neurons
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Vanilloid receptor (CHEMBL2096684)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
Park HG, Choi JY, Choi SH, Park MK, Lee J, Suh YG, Cho H, Oh U, Kim HD, Joo YH, Kim SY, Park YH, Jeong YS, Choi JK, Kim JK, Jew SS.
Bioorg Med Chem Lett (2004) 14 : 1693 -1696
PubMed 15026052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.59 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46233 1 7.82
CHEMBL48061 1 7.70
CHEMBL296963 1 7.52
CHEMBL388824 1 7.43
CHEMBL48998 1 7.22
CHEMBL45252 1 7.22
CHEMBL296729 1 7.22
CHEMBL43723 1 7.18
CHEMBL47282 1 7.16
CHEMBL431341 1 7.16
CHEMBL228451 1 6.96
CHEMBL295773 1 6.82
CHEMBL44057 1 6.66
CHEMBL45417 1 6.60
CHEMBL45455 1 6.50
CHEMBL47602 1 6.46
CHEMBL48102 1 6.30
CHEMBL47473 1 6.24
CHEMBL295302 1 6.11
CHEMBL47241 1 5.96
CHEMBL45050 1 5.70
CHEMBL47820 1 5.62
CHEMBL48338 1 5.52
CHEMBL595069 IODORESINIFERATOXIN 1 5.40
CHEMBL45817 1 4.16
CHEMBL391997 CAPSAZEPINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46233 IC50 = 15.0 nM 7.82
CHEMBL48061 IC50 = 20.0 nM 7.70
CHEMBL296963 IC50 = 30.0 nM 7.52
CHEMBL388824 IC50 = 37.0 nM 7.43
CHEMBL48998 IC50 = 60.0 nM 7.22
CHEMBL45252 IC50 = 60.0 nM 7.22
CHEMBL296729 IC50 = 60.0 nM 7.22
CHEMBL43723 IC50 = 66.0 nM 7.18
CHEMBL47282 IC50 = 70.0 nM 7.16
CHEMBL431341 IC50 = 70.0 nM 7.16
CHEMBL228451 IC50 = 110.0 nM 6.96
CHEMBL295773 IC50 = 150.0 nM 6.82
CHEMBL44057 IC50 = 220.0 nM 6.66
CHEMBL45417 IC50 = 250.0 nM 6.60
CHEMBL45455 IC50 = 320.0 nM 6.50
CHEMBL47602 IC50 = 350.0 nM 6.46
CHEMBL48102 IC50 = 500.0 nM 6.30
CHEMBL47473 IC50 = 580.0 nM 6.24
CHEMBL295302 IC50 = 770.0 nM 6.11
CHEMBL47241 IC50 = 1100.0 nM 5.96
CHEMBL45050 IC50 = 2000.0 nM 5.70
CHEMBL47820 IC50 = 2400.0 nM 5.62
CHEMBL48338 IC50 = 3000.0 nM 5.52
CHEMBL595069 IODORESINIFERATOXIN IC50 = 4000.0 nM 5.40
CHEMBL45817 IC50 = 70000.0 nM 4.16
CHEMBL391997 CAPSAZEPINE IC50 = 650.0 nM -