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Assay Detail

CHEMBL5042870

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

Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
11
Total Activities
11
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

KiSS-1 receptor (CHEMBL5413)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of an <i>N</i>-acylated-<sup>D</sup>Arg-Leu-NH<sub>2</sub> Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia.
Quillet R, Schneider S, Utard V, Drieu la Rochelle A, Elhabazi K, Henningsen JB, Gizzi P, Schmitt M, Kugler V, Simonneaux V, Ilien B, Simonin F, Bihel F.
J Med Chem (2021) 64 : 7555 -7564
PubMed 34008968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 10.21 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376756 KISSPEPTIN-10 3.0 1 10.21
CHEMBL5074999 1 -
CHEMBL5091013 1 -
CHEMBL5085324 1 -
CHEMBL4776204 1 -
CHEMBL5082678 1 -
CHEMBL1802414 1 -
CHEMBL38874 DAMGO 1 -
CHEMBL31421 1 -
CHEMBL80 NALOXONE 4.0 1 -
CHEMBL396460 NOCICEPTIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376756 KISSPEPTIN-10 Ki = 0.062 nM 10.21
CHEMBL5074999 Ki > 50000.0 nM -
CHEMBL5091013 Ki > 50000.0 nM -
CHEMBL5085324 Ki > 50000.0 nM -
CHEMBL4776204 Ki > 5000.0 nM -
CHEMBL5082678 Ki - -
CHEMBL1802414 Ki - -
CHEMBL38874 DAMGO Ki - -
CHEMBL31421 Ki - -
CHEMBL80 NALOXONE Ki - -
CHEMBL396460 NOCICEPTIN Ki - -