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Assay Detail

CHEMBL2447453

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

Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
18
Total Activities
18
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

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

Publication

Replacement of Thr32 and Gln34 in the C-terminal neuropeptide Y fragment 25-36 by cis-cyclobutane and cis-cyclopentane β-amino acids shifts selectivity toward the Y(4) receptor.
Berlicki L, Kaske M, Gutiérrez-Abad R, Bernhardt G, Illa O, Ortuño RM, Cabrele C, Buschauer A, Reiser O.
J Med Chem (2013) 56 : 8422 -8431
PubMed 24090364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.22 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438945 HUMAN NEUROPEPTIDE Y 1.0 1 8.66
CHEMBL2440192 1 7.77
CHEMBL2440199 1 -
CHEMBL2440185 1 -
CHEMBL2440186 1 -
CHEMBL2440187 1 -
CHEMBL2440188 1 -
CHEMBL2440189 1 -
CHEMBL2440190 1 -
CHEMBL2440191 1 -
CHEMBL2440200 1 -
CHEMBL2440193 1 -
CHEMBL2440194 1 -
CHEMBL2440195 1 -
CHEMBL2440196 1 -
CHEMBL2440197 1 -
CHEMBL2440198 1 -
CHEMBL2440119 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438945 HUMAN NEUROPEPTIDE Y Ki = 2.2 nM 8.66
CHEMBL2440192 Ki = 17.0 nM 7.77
CHEMBL2440199 Ki > 1000.0 nM -
CHEMBL2440185 Ki > 1000.0 nM -
CHEMBL2440186 Ki > 1000.0 nM -
CHEMBL2440187 Ki > 500.0 nM -
CHEMBL2440188 Ki > 1000.0 nM -
CHEMBL2440189 Ki > 1000.0 nM -
CHEMBL2440190 Ki > 500.0 nM -
CHEMBL2440191 Ki > 1000.0 nM -
CHEMBL2440200 Ki > 1000.0 nM -
CHEMBL2440193 Ki > 1000.0 nM -
CHEMBL2440194 Ki > 1000.0 nM -
CHEMBL2440195 Ki > 500.0 nM -
CHEMBL2440196 Ki > 1000.0 nM -
CHEMBL2440197 Ki > 1000.0 nM -
CHEMBL2440198 Ki > 1000.0 nM -
CHEMBL2440119 Ki > 1000.0 nM -