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Assay Detail

CHEMBL1291654

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

Binding
Inhibition of GCP2 by top scintillation counter in presence of 30 nM NAA[3]G
17
Total Activities
17
Compounds Tested
2
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

The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II.
Grella B, Adams J, Berry JF, Delahanty G, Ferraris DV, Majer P, Ni C, Shukla K, Shuler SA, Slusher BS, Stathis M, Tsukamoto T.
Bioorg Med Chem Lett (2010) 20 : 7222 -7225
PubMed 21074428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.54 7.82
Ki 1 11.00 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510924 1 11.00
CHEMBL382398 1 7.82
CHEMBL1288229 1 7.66
CHEMBL1288230 1 7.66
CHEMBL1287900 1 7.66
CHEMBL1288286 1 7.47
CHEMBL1288259 1 7.27
CHEMBL303352 1 7.05
CHEMBL1287842 1 7.03
CHEMBL1288258 1 7.03
CHEMBL1288287 1 6.85
CHEMBL1288536 1 5.92
CHEMBL1287872 1 5.77
CHEMBL1287873 1 5.21
CHEMBL1288228 1 4.92
CHEMBL1287871 1 4.70
CHEMBL1287843 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510924 Ki = 0.01 nM 11.00
CHEMBL382398 IC50 = 15.0 nM 7.82
CHEMBL1288229 IC50 = 22.0 nM 7.66
CHEMBL1288230 IC50 = 22.0 nM 7.66
CHEMBL1287900 IC50 = 22.0 nM 7.66
CHEMBL1288286 IC50 = 34.0 nM 7.47
CHEMBL1288259 IC50 = 54.0 nM 7.27
CHEMBL303352 IC50 = 90.0 nM 7.05
CHEMBL1287842 IC50 = 93.0 nM 7.03
CHEMBL1288258 IC50 = 94.0 nM 7.03
CHEMBL1288287 IC50 = 140.0 nM 6.85
CHEMBL1288536 IC50 = 1200.0 nM 5.92
CHEMBL1287872 IC50 = 1700.0 nM 5.77
CHEMBL1287873 IC50 = 6100.0 nM 5.21
CHEMBL1288228 IC50 = 12000.0 nM 4.92
CHEMBL1287871 IC50 = 20000.0 nM 4.70
CHEMBL1287843 IC50 = 24000.0 nM 4.62