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Assay Detail

CHEMBL680919

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

Binding
In vitro inhibitory activity against glutamate carboxypeptidase II (GCP II) using N-acetyl-L-aspartyl-[3H]L-glutamate as a substrate
2
Total Activities
2
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 (CHEMBL1892)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Majer P, Jackson PF, Delahanty G, Grella BS, Ko YS, Li W, Liu Q, Maclin KM, Poláková J, Shaffer KA, Stoermer D, Vitharana D, Wang EY, Zakrzewski A, Rojas C, Slusher BS, Wozniak KM, Burak E, Limsakun T, Tsukamoto T.
J Med Chem (2003) 46 : 1989 -1996
PubMed 12723961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.83 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47009 1 9.70
CHEMBL58957 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47009 Ki = 0.2 nM 9.70
CHEMBL58957 Ki = 11.0 nM 7.96