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Assay Detail

CHEMBL3533357

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

Binding
Inhibition of GCP-2 (unknown origin)
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate carboxypeptidase 2 (CHEMBL1892)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo.
Rais R, Hoover R, Wozniak K, Rudek MA, Tsukamoto T, Alt J, Rojas C, Slusher BS.
Drug Metab Dispos (2012) 40 : 2315 -2323
PubMed 22949627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.29 9.52
Ki 1 9.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47009 1 9.52
CHEMBL2152561 1 9.00
CHEMBL303352 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47009 IC50 = 0.3 nM 9.52
CHEMBL2152561 Ki = 1.0 nM 9.00
CHEMBL303352 IC50 = 90.0 nM 7.05