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Assay Detail

CHEMBL5247267

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Binding
Antagonist activity at rat TRPV1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design.
Subbaiah MAM, Meanwell NA.
J Med Chem (2021) 64 : 14046 -14128
PubMed 34591488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.40 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229430 AMG-517 1.0 1 9.05
CHEMBL226574 1 8.43
CHEMBL229431 1 7.57
CHEMBL229432 1 6.48
CHEMBL375460 1 6.46
CHEMBL227209 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229430 AMG-517 IC50 = 0.9 nM 9.05
CHEMBL226574 IC50 = 3.7 nM 8.43
CHEMBL229431 IC50 = 27.0 nM 7.57
CHEMBL229432 IC50 = 330.0 nM 6.48
CHEMBL375460 IC50 = 350.0 nM 6.46
CHEMBL227209 IC50 = 380.0 nM 6.42