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Assay Detail

CHEMBL783653

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Functional
Inhibition of [Ca2+] uptake in dorsal root ganglion (DRG) neurons from neonatal Sprague-Dawley rat
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vanilloid receptor (CHEMBL2096684)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects.
Suh YG, Lee YS, Min KH, Park OH, Seung HS, Kim HD, Park HG, Choi J, Lee J, Kang SW, Oh UT, Koo JY, Joo YH, Kim SY, Kim JK, Park YH.
Bioorg Med Chem Lett (2003) 13 : 4389 -4393
PubMed 14643332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.31 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388824 1 7.43
CHEMBL228451 1 6.96
CHEMBL391997 CAPSAZEPINE 1 6.23
CHEMBL136158 1 4.61
CHEMBL137697 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388824 IC50 = 37.0 nM 7.43
CHEMBL228451 IC50 = 110.0 nM 6.96
CHEMBL391997 CAPSAZEPINE IC50 = 590.0 nM 6.23
CHEMBL136158 IC50 = 24300.0 nM 4.61
CHEMBL137697 IC50 > 30000.0 nM -