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Assay Detail

CHEMBL3425009

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

Binding
Displacement of [3H]-Substance P from human NK1R after 90 mins by scintillation counting analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Substance-P receptor (CHEMBL249)
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 8 5.49 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346178 OSANETANT 2.0 1 6.40
CHEMBL437797 NEUROKININ B 1 6.30
CHEMBL3422009 1 5.90
CHEMBL3422015 1 5.10
CHEMBL3422010 1 4.90
CHEMBL3422018 1 4.90
CHEMBL10188 TALNETANT 2.0 1 4.90
CHEMBL106124 SENKTIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346178 OSANETANT Ki = 398.11 nM 6.40
CHEMBL437797 NEUROKININ B Ki = 501.19 nM 6.30
CHEMBL3422009 Ki = 1258.93 nM 5.90
CHEMBL3422015 Ki = 7943.28 nM 5.10
CHEMBL3422010 Ki = 12589.25 nM 4.90
CHEMBL3422018 Ki = 12589.25 nM 4.90
CHEMBL10188 TALNETANT Ki = 12589.25 nM 4.90
CHEMBL106124 SENKTIDE Ki > 10000.0 nM -