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Assay Detail

CHEMBL3425007

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

Binding
Displacement of [3H]-SB222200 from monkey NK3R after 90 mins by scintillation counting analysis
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NK-3 receptor (CHEMBL3421526)
Type SINGLE PROTEIN
Organism Macaca mulatta

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 5 8.02 8.40
pKi 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422009 1 8.40
CHEMBL3422015 1 8.20
CHEMBL3422018 1 8.20
CHEMBL3422010 1 7.70
CHEMBL3422017 1 7.60
CHEMBL437797 NEUROKININ B 1 -
CHEMBL106124 SENKTIDE 1 -
CHEMBL346178 OSANETANT 2.0 1 -
CHEMBL10188 TALNETANT 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422009 Ki = 3.981 nM 8.40
CHEMBL3422015 Ki = 6.31 nM 8.20
CHEMBL3422018 Ki = 6.31 nM 8.20
CHEMBL3422010 Ki = 19.95 nM 7.70
CHEMBL3422017 Ki = 25.12 nM 7.60
CHEMBL437797 NEUROKININ B pKi - -
CHEMBL106124 SENKTIDE pKi - -
CHEMBL346178 OSANETANT pKi - -
CHEMBL10188 TALNETANT pKi - -