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Assay Detail

CHEMBL1074028

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Binding
Inhibition of rat Y5 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide Y receptor type 5 (CHEMBL2548)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist.
Haga Y, Sakamoto T, Shibata T, Nonoshita K, Ishikawa M, Suga T, Takahashi H, Takahashi T, Takahashi H, Ando M, Murai T, Gomori A, Oda Z, Kitazawa H, Mitobe Y, Kanesaka M, Ohe T, Iwaasa H, Ishii Y, Ishihara A, Kanatani A, Fukami T.
Bioorg Med Chem (2009) 17 : 6971 -6982
PubMed 19720539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.62 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594163 1 8.77
CHEMBL595573 MK-0557 3.0 1 8.68
CHEMBL595790 1 8.68
CHEMBL595560 1 8.66
CHEMBL594156 1 8.60
CHEMBL595120 1 8.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594163 IC50 = 1.7 nM 8.77
CHEMBL595573 MK-0557 IC50 = 2.1 nM 8.68
CHEMBL595790 IC50 = 2.1 nM 8.68
CHEMBL595560 IC50 = 2.2 nM 8.66
CHEMBL594156 IC50 = 2.5 nM 8.60
CHEMBL595120 IC50 = 4.7 nM 8.33