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Assay Detail

CHEMBL956810

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

Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.
Sato N, Jitsuoka M, Ishikawa S, Nagai K, Tsuge H, Ando M, Okamoto O, Iwaasa H, Gomori A, Ishihara A, Kanatani A, Fukami T.
Bioorg Med Chem Lett (2009) 19 : 1670 -1674
PubMed 19233647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522456 1 8.70
CHEMBL523819 1 8.57
CHEMBL492594 1 8.37
CHEMBL490937 1 8.37
CHEMBL451113 1 8.32
CHEMBL494398 1 8.32
CHEMBL492778 1 8.27
CHEMBL492388 1 8.21
CHEMBL495034 1 8.14
CHEMBL492377 1 8.09
CHEMBL522539 1 8.06
CHEMBL495369 1 8.04
CHEMBL522489 1 8.00
CHEMBL523339 1 7.77
CHEMBL499973 1 7.52
CHEMBL493971 1 7.50
CHEMBL492766 1 7.41
CHEMBL523364 1 7.36
CHEMBL495036 1 7.33
CHEMBL522513 1 7.29
CHEMBL494175 1 7.27
CHEMBL493970 1 7.27
CHEMBL493998 1 7.23
CHEMBL506812 1 7.03
CHEMBL492779 1 6.89
CHEMBL494018 1 6.80
CHEMBL521862 1 6.80
CHEMBL522866 1 6.80
CHEMBL493997 1 6.57
CHEMBL494174 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522456 IC50 = 2.0 nM 8.70
CHEMBL523819 IC50 = 2.7 nM 8.57
CHEMBL492594 IC50 = 4.3 nM 8.37
CHEMBL490937 IC50 = 4.3 nM 8.37
CHEMBL451113 IC50 = 4.8 nM 8.32
CHEMBL494398 IC50 = 4.8 nM 8.32
CHEMBL492778 IC50 = 5.4 nM 8.27
CHEMBL492388 IC50 = 6.2 nM 8.21
CHEMBL495034 IC50 = 7.2 nM 8.14
CHEMBL492377 IC50 = 8.1 nM 8.09
CHEMBL522539 IC50 = 8.7 nM 8.06
CHEMBL495369 IC50 = 9.2 nM 8.04
CHEMBL522489 IC50 = 10.0 nM 8.00
CHEMBL523339 IC50 = 17.0 nM 7.77
CHEMBL499973 IC50 = 30.0 nM 7.52
CHEMBL493971 IC50 = 32.0 nM 7.50
CHEMBL492766 IC50 = 39.0 nM 7.41
CHEMBL523364 IC50 = 44.0 nM 7.36
CHEMBL495036 IC50 = 47.0 nM 7.33
CHEMBL522513 IC50 = 51.0 nM 7.29
CHEMBL494175 IC50 = 54.0 nM 7.27
CHEMBL493970 IC50 = 54.0 nM 7.27
CHEMBL493998 IC50 = 59.0 nM 7.23
CHEMBL506812 IC50 = 93.0 nM 7.03
CHEMBL492779 IC50 = 130.0 nM 6.89
CHEMBL494018 IC50 = 160.0 nM 6.80
CHEMBL521862 IC50 = 160.0 nM 6.80
CHEMBL522866 IC50 = 160.0 nM 6.80
CHEMBL493997 IC50 = 270.0 nM 6.57
CHEMBL494174 IC50 = 300.0 nM 6.52
CHEMBL522192 IC50 = 350.0 nM 6.46
CHEMBL523338 IC50 = 560.0 nM 6.25
CHEMBL521844 IC50 = 630.0 nM 6.20
CHEMBL522183 IC50 > 1000.0 nM -