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Assay Detail

CHEMBL812236

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

Binding
Inhibitory activity against Tachykinin receptor 1 in guinea pig 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
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Substance-P receptor (CHEMBL3942)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 8.65 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 9.40
CHEMBL353093 1 9.06
CHEMBL131171 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 IC50 = 0.4 nM 9.40
CHEMBL353093 IC50 = 0.88 nM 9.06
CHEMBL131171 IC50 = 32.0 nM 7.50