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Assay Detail

CHEMBL3102685

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Binding
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of RTX-induced 45Ca2+ uptake after 20 mins by liquid scintillation counting analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands.
Kim MS, Ki Y, Ahn SY, Yoon S, Kim SE, Park HG, Sun W, Son K, Cui M, Choi S, Pearce LV, Esch TE, Deandrea-Lazarus IA, Blumberg PM, Lee J.
Bioorg Med Chem Lett (2014) 24 : 382 -385
PubMed 24321344 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.24 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595069 IODORESINIFERATOXIN 1 8.23
CHEMBL3099610 1 7.03
CHEMBL253392 1 6.91
CHEMBL3099611 1 6.79
CHEMBL3099609 1 -
CHEMBL3099608 1 -
CHEMBL392584 1 -
CHEMBL17976 RESINIFERATOXIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595069 IODORESINIFERATOXIN Ki = 5.9 nM 8.23
CHEMBL3099610 Ki = 94.0 nM 7.03
CHEMBL253392 Ki = 122.0 nM 6.91
CHEMBL3099611 Ki = 161.0 nM 6.79
CHEMBL3099609 Ki - -
CHEMBL3099608 Ki - -
CHEMBL392584 Ki - -
CHEMBL17976 RESINIFERATOXIN Ki - -