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Assay Detail

CHEMBL5040272

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

Functional
Antagonist activity at NK1R (unknown origin) in presence of endogenous SP ligand preincubated for 10 mins followed by 30 min incubation with antagonist and SP by HTRF-FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
Recio R, Lerena P, Pozo E, Calderón-Montaño JM, Burgos-Morón E, López-Lázaro M, Valdivia V, Pernia Leal M, Mouillac B, Organero JÁ, Khiar N, Fernández I.
J Med Chem (2021) 64 : 10350 -10370
PubMed 34236855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.84 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1471 APREPITANT 4.0 1 8.85
CHEMBL5083565 1 6.45
CHEMBL5078626 1 6.08
CHEMBL5074991 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1471 APREPITANT IC50 = 1.41 nM 8.85
CHEMBL5083565 IC50 = 353.0 nM 6.45
CHEMBL5078626 IC50 = 833.0 nM 6.08
CHEMBL5074991 IC50 = 1100.0 nM 5.96