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Assay Detail

CHEMBL1259936

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Functional
Antagonist activity at human NPY Y5 receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists.
Leslie CP, Bentley J, Biagetti M, Contini S, Di Fabio R, Donati D, Genski T, Guery S, Mazzali A, Merlo G, Pizzi DA, Sacco F, Seri C, Tessari M, Zonzini L, Caberlotto L.
Bioorg Med Chem Lett (2010) 20 : 6103 -6107
PubMed 20813523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 9.67 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1257993 1 10.60
CHEMBL1258111 1 10.50
CHEMBL1258225 1 10.40
CHEMBL1258787 1 10.20
CHEMBL1257992 1 10.20
CHEMBL1258341 1 10.20
CHEMBL1258110 1 10.10
CHEMBL1258340 1 10.00
CHEMBL1258674 1 10.00
CHEMBL1258453 1 10.00
CHEMBL1257636 1 10.00
CHEMBL1257637 1 9.90
CHEMBL1257761 1 9.80
CHEMBL1258673 1 9.80
CHEMBL1257760 1 9.80
CHEMBL1258454 1 9.70
CHEMBL1258562 1 9.70
CHEMBL1258788 1 9.60
CHEMBL1258224 1 9.50
CHEMBL1258907 1 9.50
CHEMBL1257520 1 9.20
CHEMBL1257881 1 9.00
CHEMBL1258563 1 8.80
CHEMBL1257173 1 8.70
CHEMBL1257882 1 8.30
CHEMBL1209347 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1257993 Ki = 0.02512 nM 10.60
CHEMBL1258111 Ki = 0.03162 nM 10.50
CHEMBL1258225 Ki = 0.03981 nM 10.40
CHEMBL1258787 Ki = 0.0631 nM 10.20
CHEMBL1257992 Ki = 0.0631 nM 10.20
CHEMBL1258341 Ki = 0.0631 nM 10.20
CHEMBL1258110 Ki = 0.07943 nM 10.10
CHEMBL1258340 Ki = 0.1 nM 10.00
CHEMBL1258674 Ki = 0.1 nM 10.00
CHEMBL1258453 Ki = 0.1 nM 10.00
CHEMBL1257636 Ki = 0.1 nM 10.00
CHEMBL1257637 Ki = 0.1259 nM 9.90
CHEMBL1257761 Ki = 0.1585 nM 9.80
CHEMBL1258673 Ki = 0.1585 nM 9.80
CHEMBL1257760 Ki = 0.1585 nM 9.80
CHEMBL1258454 Ki = 0.1995 nM 9.70
CHEMBL1258562 Ki = 0.1995 nM 9.70
CHEMBL1258788 Ki = 0.2512 nM 9.60
CHEMBL1258224 Ki = 0.3162 nM 9.50
CHEMBL1258907 Ki = 0.3162 nM 9.50
CHEMBL1257520 Ki = 0.631 nM 9.20
CHEMBL1257881 Ki = 1.0 nM 9.00
CHEMBL1258563 Ki = 1.585 nM 8.80
CHEMBL1257173 Ki = 1.995 nM 8.70
CHEMBL1257882 Ki = 5.012 nM 8.30
CHEMBL1209347 Ki = 15.85 nM 7.80