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Assay Detail

CHEMBL814665

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

Binding
Inhibitory activity against Tachykinin receptor 1 in mouse brain using [125I]-labeled Boltan-Hunter substance P as radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL2668)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
Hipskind PA, Howbert JJ, Bruns RF, Cho SS, Crowell TA, Foreman MM, Gehlert DR, Iyengar S, Johnson KW, Krushinski JH, Li DL, Lobb KL, Mason NR, Muehl BS, Nixon JA, Phebus LA, Regoli D, Simmons RM, Threlkeld PG, Waters DC, Gitter BD.
J Med Chem (1996) 39 : 736 -748
PubMed 8576917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.88 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348976 1 8.89
CHEMBL131171 1 8.06
CHEMBL350151 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348976 IC50 = 1.3 nM 8.89
CHEMBL131171 IC50 = 8.7 nM 8.06
CHEMBL350151 IC50 = 200.0 nM 6.70