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Assay Detail

CHEMBL857548

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

Binding
Compound was tested for inhibition of NK1 receptor from gerbil midbrain
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gerbillinae
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist
Ofner S, Hauser K, Schilling W, Vassout A, Veenstra SJ
Bioorg Med Chem Lett (1996) 6 : 1623 -1628
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.98 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43912 1 7.32
CHEMBL290364 1 7.26
CHEMBL295122 1 7.16
CHEMBL297883 1 6.16
CHEMBL295425 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43912 IC50 = 48.0 nM 7.32
CHEMBL290364 IC50 = 55.0 nM 7.26
CHEMBL295122 IC50 = 70.0 nM 7.16
CHEMBL297883 IC50 = 690.0 nM 6.16
CHEMBL295425 IC50 = 10.0 -