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Assay Detail

CHEMBL5116484

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

Binding
Inhibition of PSMA in human LNCaP cell extracts using NAAG as substrate by amplex red reagent based assay
17
Total Activities
17
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

Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.
Zyk NY, Ber AP, Nimenko EA, Shafikov RR, Evteev SA, Petrov SA, Uspenskaya AA, Dashkova NS, Ivanenkov YA, Skvortsov DA, Beloglazkina EK, Majouga AG, Machulkin AE.
Bioorg Med Chem Lett (2022) 71 : 128840 -128840
PubMed 35661685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.56 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5205430 1 8.82
CHEMBL5202039 1 8.68
CHEMBL5204026 1 8.15
CHEMBL596351 1 7.96
CHEMBL5182529 1 7.80
CHEMBL5204600 1 7.72
CHEMBL5187511 1 7.64
CHEMBL5171332 1 7.64
CHEMBL5184954 1 7.62
CHEMBL5183648 1 7.46
CHEMBL5202319 1 7.42
CHEMBL5182330 1 7.29
CHEMBL189217 1 7.10
CHEMBL5206416 1 7.06
CHEMBL5194802 1 7.00
CHEMBL5203501 1 6.95
CHEMBL458202 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5205430 IC50 = 1.5 nM 8.82
CHEMBL5202039 IC50 = 2.1 nM 8.68
CHEMBL5204026 IC50 = 7.0 nM 8.15
CHEMBL596351 IC50 = 11.0 nM 7.96
CHEMBL5182529 IC50 = 16.0 nM 7.80
CHEMBL5204600 IC50 = 19.0 nM 7.72
CHEMBL5187511 IC50 = 23.0 nM 7.64
CHEMBL5171332 IC50 = 23.0 nM 7.64
CHEMBL5184954 IC50 = 24.0 nM 7.62
CHEMBL5183648 IC50 = 35.0 nM 7.46
CHEMBL5202319 IC50 = 38.0 nM 7.42
CHEMBL5182330 IC50 = 51.0 nM 7.29
CHEMBL189217 IC50 = 80.0 nM 7.10
CHEMBL5206416 IC50 = 88.0 nM 7.06
CHEMBL5194802 IC50 = 101.0 nM 7.00
CHEMBL5203501 IC50 = 112.0 nM 6.95
CHEMBL458202 IC50 = 547.0 nM 6.26