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Assay Detail

CHEMBL1647472

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

Binding
Displacement of [3H]RTX from rat TRV1 expressed in CHO cells by competitive binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Receptor activity and conformational analysis of 5'-halogenated resiniferatoxin analogs as TRPV1 ligands.
Lim KS, Kang DW, Kim YS, Kim MS, Park SG, Choi S, Pearce LV, Blumberg PM, Lee J.
Bioorg Med Chem Lett (2011) 21 : 299 -302
PubMed 21111618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 9.20 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17976 RESINIFERATOXIN 3.0 1 10.37
CHEMBL1644419 1 9.89
CHEMBL1644416 1 9.77
CHEMBL1644414 1 9.59
CHEMBL1644417 1 9.52
CHEMBL1644413 1 9.21
CHEMBL1644420 1 9.15
CHEMBL1644421 1 9.07
CHEMBL1644415 1 8.99
CHEMBL1644422 1 8.70
CHEMBL1644418 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17976 RESINIFERATOXIN Ki = 0.043 nM 10.37
CHEMBL1644419 Ki = 0.13 nM 9.89
CHEMBL1644416 Ki = 0.17 nM 9.77
CHEMBL1644414 Ki = 0.26 nM 9.59
CHEMBL1644417 Ki = 0.3 nM 9.52
CHEMBL1644413 Ki = 0.61 nM 9.21
CHEMBL1644420 Ki = 0.7 nM 9.15
CHEMBL1644421 Ki = 0.85 nM 9.07
CHEMBL1644415 Ki = 1.03 nM 8.99
CHEMBL1644422 Ki = 1.99 nM 8.70
CHEMBL1644418 Ki = 110.0 nM 6.96