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Assay Detail

CHEMBL4265264

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

ADMET
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y1R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Mus musculus
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design of Y2 Receptor Selective and Proteolytically Stable PYY3-36 Analogues.
Østergaard S, Kofoed J, Paulsson JF, Madsen KG, Jorgensen R, Wulff BS.
J Med Chem (2018) 61 : 10519 -10530
PubMed 30399314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.28 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281479 2 9.70
CHEMBL4276961 2 8.00
CHEMBL4292105 2 7.30
CHEMBL4280392 2 6.20
CHEMBL4290445 2 5.20
CHEMBL4287058 2 -
CHEMBL4283257 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281479 EC50 = 0.2 nM 9.70
CHEMBL4281479 EC50 = 0.1995 nM 9.70
CHEMBL4276961 EC50 = 10.0 nM 8.00
CHEMBL4276961 EC50 = 10.0 nM 8.00
CHEMBL4292105 EC50 = 50.0 nM 7.30
CHEMBL4292105 EC50 = 50.12 nM 7.30
CHEMBL4280392 EC50 = 630.0 nM 6.20
CHEMBL4280392 EC50 = 630.96 nM 6.20
CHEMBL4290445 EC50 = 6300.0 nM 5.20
CHEMBL4290445 EC50 = 6309.57 nM 5.20
CHEMBL4287058 EC50 > 10000.0 nM -
CHEMBL4287058 EC50 > 10000.0 nM -
CHEMBL4283257 EC50 > 10000.0 nM -
CHEMBL4283257 EC50 > 10000.0 nM -