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Assay Detail

CHEMBL3425266

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

Binding
Displacement of [125I][MePhe7]NKB from human NK3R expressed in CHO cell membranes after 90 mins by scintillation counting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuromedin-K receptor (CHEMBL4429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
Hoveyda HR, Fraser GL, Roy MO, Dutheuil G, Batt F, El Bousmaqui M, Korac J, Lenoir F, Lapin A, Noël S, Blanc S.
J Med Chem (2015) 58 : 3060 -3082
PubMed 25738882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.80 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437797 NEUROKININ B 1 9.10
CHEMBL106124 SENKTIDE 1 8.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437797 NEUROKININ B Ki = 0.7943 nM 9.10
CHEMBL106124 SENKTIDE Ki = 3.162 nM 8.50