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Assay Detail

CHEMBL5522869

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

Binding
Binding affinity to PREP Leu499Cys mutant (unknown origin) assessed as binding constant by ITC analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein-Protein Interaction-Derived Functions.
Pätsi HT, Kilpeläinen TP, Jumppanen M, Uhari-Väänänen J, Wielendaele PV, De Lorenzo F, Cui H, Auno S, Saharinen J, Seppälä E, Sipari N, Savinainen J, De Meester I, Lambeir AM, Lahtela-Kakkonen M, Myöhänen TT, Wallén EAA.
J Med Chem (2024) 67 : 5421 -5436
PubMed 38546708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 6.41 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL435223 1 7.09
CHEMBL5563880 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL435223 Kd = 82.0 nM 7.09
CHEMBL5563880 Kd = 1863.0 nM 5.73