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Assay Detail

CHEMBL832980

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Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
13
Total Activities
13
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

Discovery of 4-(dimethylamino)quinazolines as 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, Beeley N, Sekiguchi Y.
Bioorg Med Chem Lett (2005) 15 : 2565 -2569
PubMed 15863317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.35 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17645 CGP-71683A 1 8.89
CHEMBL192266 1 8.80
CHEMBL193970 1 8.60
CHEMBL193438 1 8.57
CHEMBL193666 1 8.31
CHEMBL193771 1 7.51
CHEMBL195123 1 7.39
CHEMBL425012 1 7.11
CHEMBL195810 1 6.92
CHEMBL194602 1 6.82
CHEMBL195346 1 6.06
CHEMBL194173 1 5.52
CHEMBL360671 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17645 CGP-71683A IC50 = 1.3 nM 8.89
CHEMBL192266 IC50 = 1.6 nM 8.80
CHEMBL193970 IC50 = 2.5 nM 8.60
CHEMBL193438 IC50 = 2.7 nM 8.57
CHEMBL193666 IC50 = 4.9 nM 8.31
CHEMBL193771 IC50 = 31.0 nM 7.51
CHEMBL195123 IC50 = 41.0 nM 7.39
CHEMBL425012 IC50 = 78.0 nM 7.11
CHEMBL195810 IC50 = 120.0 nM 6.92
CHEMBL194602 IC50 = 150.0 nM 6.82
CHEMBL195346 IC50 = 880.0 nM 6.06
CHEMBL194173 IC50 = 3000.0 nM 5.52
CHEMBL360671 IC50 = 8900.0 nM 5.05