Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL874561

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

Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Neuropeptide Y receptor type 5 (CHEMBL4561)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Kanuma K, Omodera K, Nishiguchi M, Funakoshi T, Chaki S, Semple G, Tran TA, Kramer B, Hsu D, Casper M, Thomsen B, Sekiguchi Y.
Bioorg Med Chem Lett (2005) 15 : 3853 -3856
PubMed 16002290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.25 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL537846 1 8.57
CHEMBL181217 1 6.92
CHEMBL181727 1 6.34
CHEMBL367355 1 6.33
CHEMBL360117 1 6.25
CHEMBL180003 1 6.06
CHEMBL181393 1 5.75
CHEMBL181466 1 5.62
CHEMBL182150 1 5.57
CHEMBL360671 1 5.05
CHEMBL181184 1 -
CHEMBL178084 1 -
CHEMBL182235 1 -
CHEMBL360876 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL537846 IC50 = 2.7 nM 8.57
CHEMBL181217 IC50 = 120.0 nM 6.92
CHEMBL181727 IC50 = 460.0 nM 6.34
CHEMBL367355 IC50 = 470.0 nM 6.33
CHEMBL360117 IC50 = 560.0 nM 6.25
CHEMBL180003 IC50 = 880.0 nM 6.06
CHEMBL181393 IC50 = 1800.0 nM 5.75
CHEMBL181466 IC50 = 2400.0 nM 5.62
CHEMBL182150 IC50 = 2700.0 nM 5.57
CHEMBL360671 IC50 = 8900.0 nM 5.05
CHEMBL181184 IC50 > 1000.0 nM -
CHEMBL178084 IC50 > 1000.0 nM -
CHEMBL182235 IC50 > 1000.0 nM -
CHEMBL360876 IC50 > 1000.0 nM -