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Assay Detail

CHEMBL818740

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

Functional
Antagonistic activity against vanilloid receptor as concentration to reduce the response to 0.5 mM capsaicin by 50% from neonatal rat culture spinal sensory neurons using [Ca2+] -influx assay
23
Total Activities
22
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

Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.
Park HG, Park MK, Choi JY, Choi SH, Lee J, Park BS, Kim MG, Suh YG, Cho H, Oh U, Lee J, Kim HD, Park YH, Koh HJ, Lim KM, Moh JH, Jew SS.
Bioorg Med Chem Lett (2003) 13 : 601 -604
PubMed 12639539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.72 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415543 2 9.49
CHEMBL155433 1 9.34
CHEMBL154743 1 9.30
CHEMBL156041 1 9.26
CHEMBL267205 1 9.14
CHEMBL155730 1 9.02
CHEMBL154990 1 9.02
CHEMBL157962 1 8.92
CHEMBL422702 1 8.62
CHEMBL434295 1 8.60
CHEMBL156693 1 8.52
CHEMBL356682 1 8.49
CHEMBL157917 1 8.29
CHEMBL158189 1 8.21
CHEMBL156927 1 8.03
CHEMBL345157 1 8.00
CHEMBL157918 1 7.98
CHEMBL157579 1 7.92
CHEMBL157688 1 -
CHEMBL348634 1 -
CHEMBL391997 CAPSAZEPINE 1 -
CHEMBL157473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415543 IC50 = 0.32 nM 9.49
CHEMBL415543 IC50 = 0.32 nM 9.49
CHEMBL155433 IC50 = 0.46 nM 9.34
CHEMBL154743 IC50 = 0.5 nM 9.30
CHEMBL156041 IC50 = 0.55 nM 9.26
CHEMBL267205 IC50 = 0.72 nM 9.14
CHEMBL154990 IC50 = 0.95 nM 9.02
CHEMBL155730 IC50 = 0.95 nM 9.02
CHEMBL157962 IC50 = 1.2 nM 8.92
CHEMBL422702 IC50 = 2.4 nM 8.62
CHEMBL434295 IC50 = 2.5 nM 8.60
CHEMBL156693 IC50 = 3.0 nM 8.52
CHEMBL356682 IC50 = 3.2 nM 8.49
CHEMBL157917 IC50 = 5.1 nM 8.29
CHEMBL158189 IC50 = 6.1 nM 8.21
CHEMBL156927 IC50 = 9.3 nM 8.03
CHEMBL345157 IC50 = 10.0 nM 8.00
CHEMBL157918 IC50 = 10.5 nM 7.98
CHEMBL157579 IC50 = 12.0 nM 7.92
CHEMBL391997 CAPSAZEPINE IC50 = 650000.0 nM -
CHEMBL157688 IC50 > 30.0 nM -
CHEMBL157473 IC50 > 30.0 nM -
CHEMBL348634 IC50 > 30.0 nM -