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Assay Detail

CHEMBL4841968

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Binding
Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis
ChEMBL ↗
50
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuropeptide Y receptor type 4 (CHEMBL4877) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y<sub>4</sub> Receptor Ligands Results in Picomolar Binding Constants.
Konieczny A, Conrad M, Ertl FJ, Gleixner J, Gattor AO, Grätz L, Schmidt MF, Neu E, Horn AHC, Wifling D, Gmeiner P, Clark T, Sticht H, Keller M.
J Med Chem (2021) 64 : 16746 -16769
PubMed 34748345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 46 8.47 10.48
pKi 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4856311 — — 2 10.48
CHEMBL4873376 — — 2 10.36
CHEMBL4857577 — — 2 9.93
CHEMBL4848958 — — 2 9.63
CHEMBL4860290 — — 2 9.19
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 2 9.16
CHEMBL4865048 — — 2 8.90
CHEMBL4866086 — — 2 8.85
CHEMBL4852799 — — 2 8.80
CHEMBL4870168 — — 2 8.71
CHEMBL4858915 — — 2 8.60
CHEMBL4633593 — — 2 8.47
CHEMBL4862140 — — 2 8.16
CHEMBL4877802 — — 2 8.00
CHEMBL4874445 — — 2 7.55
CHEMBL4852354 — — 2 7.54
CHEMBL4863955 — — 2 7.30
CHEMBL4868787 — — 2 7.30
CHEMBL4874850 — — 2 7.25
CHEMBL4861544 — — 2 6.87
CHEMBL4866955 — — 2 6.86
CHEMBL4632871 — — 2 -
CHEMBL4863428 — — 2 -
CHEMBL4847157 — — 2 -
CHEMBL4639709 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4856311 — Ki = 0.03311 nM 10.48
CHEMBL4856311 — Ki = 0.033 nM 10.48
CHEMBL4873376 — Ki = 0.04365 nM 10.36
CHEMBL4873376 — Ki = 0.048 nM 10.32
CHEMBL4857577 — Ki = 0.1175 nM 9.93
CHEMBL4857577 — Ki = 0.13 nM 9.89
CHEMBL4848958 — Ki = 0.2344 nM 9.63
CHEMBL4848958 — Ki = 0.24 nM 9.62
CHEMBL4860290 — Ki = 0.6457 nM 9.19
CHEMBL4860290 — Ki = 0.66 nM 9.18
CHEMBL4540843 PANCREATIC POLYPEPTIDE Ki = 0.6918 nM 9.16
CHEMBL4540843 PANCREATIC POLYPEPTIDE Ki = 0.69 nM 9.16
CHEMBL4865048 — Ki = 1.259 nM 8.90
CHEMBL4866086 — Ki = 1.4 nM 8.85
CHEMBL4866086 — Ki = 1.413 nM 8.85
CHEMBL4852799 — Ki = 1.585 nM 8.80
CHEMBL4852799 — Ki = 1.6 nM 8.80
CHEMBL4870168 — Ki = 1.95 nM 8.71
CHEMBL4870168 — Ki = 2.1 nM 8.68
CHEMBL4858915 — Ki = 2.512 nM 8.60
CHEMBL4858915 — Ki = 2.5 nM 8.60
CHEMBL4633593 — Ki = 3.388 nM 8.47
CHEMBL4862140 — Ki = 6.918 nM 8.16
CHEMBL4862140 — Ki = 7.1 nM 8.15
CHEMBL4877802 — Ki = 10.0 nM 8.00
CHEMBL4877802 — Ki = 10.23 nM 7.99
CHEMBL4865048 — Ki = 13.0 nM 7.89
CHEMBL4874445 — Ki = 28.0 nM 7.55
CHEMBL4874445 — Ki = 28.84 nM 7.54
CHEMBL4852354 — Ki = 28.84 nM 7.54
CHEMBL4852354 — Ki = 30.0 nM 7.52
CHEMBL4868787 — Ki = 50.12 nM 7.30
CHEMBL4863955 — Ki = 50.0 nM 7.30
CHEMBL4868787 — Ki = 53.0 nM 7.28
CHEMBL4874850 — Ki = 56.23 nM 7.25
CHEMBL4874850 — Ki = 63.0 nM 7.20
CHEMBL4861544 — Ki = 134.9 nM 6.87
CHEMBL4866955 — Ki = 138.04 nM 6.86
CHEMBL4861544 — Ki = 140.0 nM 6.85
CHEMBL4866955 — Ki = 170.0 nM 6.77
CHEMBL4633593 — Ki - — -
CHEMBL4632871 — pKi - — -
CHEMBL4639709 — Ki - — -
CHEMBL4863428 — pKi - — -
CHEMBL4847157 — pKi - — -
CHEMBL4639709 — pKi - — -
CHEMBL4847157 — Ki - — -
CHEMBL4863428 — Ki - — -
CHEMBL4632871 — Ki - — -
CHEMBL4863955 — Ki = 736.0 nM -