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Assay Detail

CHEMBL1004546

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

Binding
Displacement of [3H]RTX form rat TRPV1 receptor expressed in CHO/VR1 cell system
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO/VR1
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.
Choi HK, Choi S, Lee Y, Kang DW, Ryu H, Maeng HJ, Chung SJ, Pavlyukovets VA, Pearce LV, Toth A, Tran R, Wang Y, Morgan MA, Blumberg PM, Lee J.
Bioorg Med Chem (2009) 17 : 690 -698
PubMed 19135377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.51 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17976 RESINIFERATOXIN 3.0 1 10.37
CHEMBL504725 1 10.14
CHEMBL503101 1 9.64
CHEMBL510583 1 9.40
CHEMBL509154 1 9.08
CHEMBL510228 1 9.05
CHEMBL449201 1 9.01
CHEMBL455555 1 8.62
CHEMBL455155 1 8.57
CHEMBL502769 1 8.51
CHEMBL509331 1 8.45
CHEMBL504206 1 8.17
CHEMBL462654 1 8.08
CHEMBL506945 1 6.87
CHEMBL500075 1 6.50
CHEMBL294199 CAPSAICIN 4.0 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17976 RESINIFERATOXIN Ki = 0.0426 nM 10.37
CHEMBL504725 Ki = 0.073 nM 10.14
CHEMBL503101 Ki = 0.228 nM 9.64
CHEMBL510583 Ki = 0.4 nM 9.40
CHEMBL509154 Ki = 0.84 nM 9.08
CHEMBL510228 Ki = 0.89 nM 9.05
CHEMBL449201 Ki = 0.98 nM 9.01
CHEMBL455555 Ki = 2.4 nM 8.62
CHEMBL455155 Ki = 2.69 nM 8.57
CHEMBL502769 Ki = 3.1 nM 8.51
CHEMBL509331 Ki = 3.53 nM 8.45
CHEMBL504206 Ki = 6.81 nM 8.17
CHEMBL462654 Ki = 8.3 nM 8.08
CHEMBL506945 Ki = 135.0 nM 6.87
CHEMBL500075 Ki = 320.0 nM 6.50
CHEMBL294199 CAPSAICIN Ki = 1808.0 nM 5.74