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Assay Detail

CHEMBL820098

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

Binding
Binding affinity towards cloned human vanilloid receptor subtype 1 in HEK293 cell membranes using [3H]RTX as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Publication

7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.
McDonnell ME, Zhang SP, Nasser N, Dubin AE, Dax SL.
Bioorg Med Chem Lett (2004) 14 : 531 -534
PubMed 14698197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.68 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147068 1 9.00
CHEMBL151298 1 9.00
CHEMBL148920 1 9.00
CHEMBL358953 1 8.70
CHEMBL151446 1 8.68
CHEMBL147028 1 8.55
CHEMBL357738 1 8.40
CHEMBL348001 1 8.34
CHEMBL342300 1 8.15
CHEMBL151442 1 8.01
CHEMBL147022 1 7.28
CHEMBL139989 1 7.03
CHEMBL391997 CAPSAZEPINE 1 6.92
CHEMBL405658 1 6.24
CHEMBL151378 1 5.96
CHEMBL440535 1 5.74
CHEMBL151657 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147068 Ki = 1.0 nM 9.00
CHEMBL151298 Ki = 1.0 nM 9.00
CHEMBL148920 Ki = 1.0 nM 9.00
CHEMBL358953 Ki = 2.0 nM 8.70
CHEMBL151446 Ki = 2.1 nM 8.68
CHEMBL147028 Ki = 2.8 nM 8.55
CHEMBL357738 Ki = 4.0 nM 8.40
CHEMBL348001 Ki = 4.6 nM 8.34
CHEMBL342300 Ki = 7.0 nM 8.15
CHEMBL151442 Ki = 9.8 nM 8.01
CHEMBL147022 Ki = 53.0 nM 7.28
CHEMBL139989 Ki = 94.0 nM 7.03
CHEMBL391997 CAPSAZEPINE Ki = 120.0 nM 6.92
CHEMBL405658 Ki = 581.0 nM 6.24
CHEMBL151378 Ki = 1110.0 nM 5.96
CHEMBL440535 Ki = 1830.0 nM 5.74
CHEMBL151657 Ki = 3280.0 nM 5.48