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Assay Detail

CHEMBL748548

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Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type AV12
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Neuropeptide Y receptor type 1 (CHEMBL4777)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.
Zarrinmayeh H, Zimmerman DM, Cantrell BE, Schober DA, Bruns RF, Gackenheimer SL, Ornstein PL, Hipskind PA, Britton TC, Gehlert DR.
Bioorg Med Chem Lett (1999) 9 : 647 -652
PubMed 10201822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 9.31 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL349328 1 10.28
CHEMBL155802 1 9.97
CHEMBL347807 1 9.95
CHEMBL439643 1 9.88
CHEMBL346243 1 9.74
CHEMBL345581 1 9.72
CHEMBL348123 1 9.54
CHEMBL156076 1 9.54
CHEMBL350917 1 9.50
CHEMBL346242 1 9.44
CHEMBL348119 1 9.41
CHEMBL434467 1 9.15
CHEMBL157661 1 9.12
CHEMBL159220 1 9.08
CHEMBL158392 1 8.79
CHEMBL347804 1 8.79
CHEMBL155925 1 8.79
CHEMBL61532 1 8.77
CHEMBL265752 1 8.35
CHEMBL145714 1 8.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL349328 Ki = 0.052 nM 10.28
CHEMBL155802 Ki = 0.106 nM 9.97
CHEMBL347807 Ki = 0.112 nM 9.95
CHEMBL439643 Ki = 0.132 nM 9.88
CHEMBL346243 Ki = 0.183 nM 9.74
CHEMBL345581 Ki = 0.191 nM 9.72
CHEMBL348123 Ki = 0.29 nM 9.54
CHEMBL156076 Ki = 0.285 nM 9.54
CHEMBL350917 Ki = 0.313 nM 9.50
CHEMBL346242 Ki = 0.361 nM 9.44
CHEMBL348119 Ki = 0.393 nM 9.41
CHEMBL434467 Ki = 0.707 nM 9.15
CHEMBL157661 Ki = 0.75 nM 9.12
CHEMBL159220 Ki = 0.829 nM 9.08
CHEMBL158392 Ki = 1.61 nM 8.79
CHEMBL347804 Ki = 1.63 nM 8.79
CHEMBL155925 Ki = 1.62 nM 8.79
CHEMBL61532 Ki = 1.7 nM 8.77
CHEMBL265752 Ki = 4.5 nM 8.35
CHEMBL145714 Ki = 4.5 nM 8.35