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Assay Detail

CHEMBL4358815

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

Binding
Inhibition of PSMA in human LNCaP cell extracts in presence of N-acetylaspartylglutamate by Amplex red glutamic acid dependent fluorescence-based NAALADase assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel β- and γ-Amino Acid-Derived Inhibitors of Prostate-Specific Membrane Antigen.
Kim K, Kwon H, Barinka C, Motlova L, Nam S, Choi D, Ha H, Nam H, Son SH, Minn I, Pomper MG, Yang X, Kutil Z, Byun Y.
J Med Chem (2020) 63 : 3261 -3273
PubMed 32097010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.63 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510924 1 9.66
CHEMBL4299851 PIFLUFOLASTAT 4.0 1 8.81
CHEMBL4590944 1 8.40
CHEMBL4461865 1 7.96
CHEMBL4513630 1 7.92
CHEMBL4445179 1 7.78
CHEMBL4471968 1 6.97
CHEMBL4466904 1 6.81
CHEMBL4558538 1 6.71
CHEMBL4586744 1 6.55
CHEMBL4457563 1 6.40
CHEMBL4453028 1 -
CHEMBL4439962 1 -
CHEMBL4550529 1 -
CHEMBL4459755 1 -
CHEMBL4459899 1 -
CHEMBL4514701 1 -
CHEMBL4588782 1 -
CHEMBL4524986 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510924 IC50 = 0.22 nM 9.66
CHEMBL4299851 PIFLUFOLASTAT IC50 = 1.56 nM 8.81
CHEMBL4590944 IC50 = 3.97 nM 8.40
CHEMBL4461865 IC50 = 11.0 nM 7.96
CHEMBL4513630 IC50 = 11.9 nM 7.92
CHEMBL4445179 IC50 = 16.7 nM 7.78
CHEMBL4471968 IC50 = 107.0 nM 6.97
CHEMBL4466904 IC50 = 155.0 nM 6.81
CHEMBL4558538 IC50 = 195.0 nM 6.71
CHEMBL4586744 IC50 = 284.0 nM 6.55
CHEMBL4457563 IC50 = 399.0 nM 6.40
CHEMBL4453028 IC50 > 1000.0 nM -
CHEMBL4439962 IC50 > 1000.0 nM -
CHEMBL4550529 IC50 > 1000.0 nM -
CHEMBL4459755 IC50 > 1000.0 nM -
CHEMBL4459899 IC50 > 1000.0 nM -
CHEMBL4514701 IC50 > 1000.0 nM -
CHEMBL4588782 IC50 > 1000.0 nM -
CHEMBL4524986 IC50 > 1000.0 nM -