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Assay Detail

CHEMBL680923

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Binding
Inhibitory activity against expressed rat Glutamate carboxypeptidase II, using a substrate concentration of 5 uM
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate carboxypeptidase 2 (CHEMBL5098)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
Kozikowski AP, Nan F, Conti P, Zhang J, Ramadan E, Bzdega T, Wroblewska B, Neale JH, Pshenichkin S, Wroblewski JT.
J Med Chem (2001) 44 : 298 -301
PubMed 11462970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.52 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47009 1 8.29
CHEMBL103512 1 8.16
CHEMBL103725 1 7.66
CHEMBL322896 1 7.54
CHEMBL46005 1 7.33
CHEMBL318315 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47009 IC50 = 5.1 nM 8.29
CHEMBL103512 IC50 = 6.9 nM 8.16
CHEMBL103725 IC50 = 21.7 nM 7.66
CHEMBL322896 IC50 = 29.0 nM 7.54
CHEMBL46005 IC50 = 47.0 nM 7.33
CHEMBL318315 IC50 = 750.0 nM 6.12