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Assay Detail

CHEMBL2020488

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

Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor.
Fichtner M, Lee E, Tomlinson E, Scott D, Cornelius P, Patterson TA, Carpino PA.
Bioorg Med Chem Lett (2012) 22 : 2738 -2743
PubMed 22445286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.95 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2016732 1 9.15
CHEMBL2016682 1 9.10
CHEMBL2016740 1 9.05
CHEMBL2016739 1 9.00
CHEMBL161724 1 8.92
CHEMBL595573 MK-0557 3.0 1 8.80
CHEMBL2016737 1 8.62
CHEMBL2016742 1 8.34
CHEMBL2016681 VELNEPERIT 2.0 1 8.30
CHEMBL2016736 1 8.10
CHEMBL2016735 1 8.00
CHEMBL2016743 1 7.96
CHEMBL2016733 1 7.66
CHEMBL2016741 1 7.09
CHEMBL2016738 1 6.73
CHEMBL2016745 1 6.52
CHEMBL2016734 1 6.07
CHEMBL2016744 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2016732 Ki = 0.7 nM 9.15
CHEMBL2016682 Ki = 0.8 nM 9.10
CHEMBL2016740 Ki = 0.9 nM 9.05
CHEMBL2016739 Ki = 1.0 nM 9.00
CHEMBL161724 Ki = 1.2 nM 8.92
CHEMBL595573 MK-0557 Ki = 1.6 nM 8.80
CHEMBL2016737 Ki = 2.4 nM 8.62
CHEMBL2016742 Ki = 4.6 nM 8.34
CHEMBL2016681 VELNEPERIT Ki = 5.0 nM 8.30
CHEMBL2016736 Ki = 8.0 nM 8.10
CHEMBL2016735 Ki = 10.0 nM 8.00
CHEMBL2016743 Ki = 11.0 nM 7.96
CHEMBL2016733 Ki = 22.0 nM 7.66
CHEMBL2016741 Ki = 82.0 nM 7.09
CHEMBL2016738 Ki = 188.0 nM 6.73
CHEMBL2016745 Ki = 301.0 nM 6.52
CHEMBL2016734 Ki = 849.0 nM 6.07
CHEMBL2016744 Ki = 2330.0 nM 5.63