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Assay Detail

CHEMBL4270348

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

Binding
Inhibition of recombinant human PSMA using [3H]NAAG as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by liquid scintillation method
20
Total Activities
20
Compounds Tested
1
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

2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.
Nakajima R, Nováková Z, Tueckmantel W, Motlová L, Bařinka C, Kozikowski AP.
ACS Med Chem Lett (2018) 9 : 1099 -1104
PubMed 30429952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 9.16 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510924 1 10.68
CHEMBL4284995 1 10.12
CHEMBL4280968 1 9.89
CHEMBL4286872 1 9.82
CHEMBL4288368 1 9.70
CHEMBL4277729 1 9.55
CHEMBL4291782 1 9.46
CHEMBL4291245 1 9.34
CHEMBL4283406 1 9.19
CHEMBL4294773 1 9.03
CHEMBL4292853 1 9.00
CHEMBL4291603 1 8.96
CHEMBL4281573 1 8.92
CHEMBL4289458 1 8.88
CHEMBL4294649 1 8.68
CHEMBL4279502 1 8.63
CHEMBL4286751 1 8.54
CHEMBL4281157 1 8.35
CHEMBL4279929 1 8.28
CHEMBL4287838 1 8.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510924 IC50 = 0.021 nM 10.68
CHEMBL4284995 IC50 = 0.075 nM 10.12
CHEMBL4280968 IC50 = 0.13 nM 9.89
CHEMBL4286872 IC50 = 0.15 nM 9.82
CHEMBL4288368 IC50 = 0.2 nM 9.70
CHEMBL4277729 IC50 = 0.28 nM 9.55
CHEMBL4291782 IC50 = 0.35 nM 9.46
CHEMBL4291245 IC50 = 0.46 nM 9.34
CHEMBL4283406 IC50 = 0.64 nM 9.19
CHEMBL4294773 IC50 = 0.94 nM 9.03
CHEMBL4292853 IC50 = 0.99 nM 9.00
CHEMBL4291603 IC50 = 1.11 nM 8.96
CHEMBL4281573 IC50 = 1.19 nM 8.92
CHEMBL4289458 IC50 = 1.31 nM 8.88
CHEMBL4294649 IC50 = 2.11 nM 8.68
CHEMBL4279502 IC50 = 2.32 nM 8.63
CHEMBL4286751 IC50 = 2.91 nM 8.54
CHEMBL4281157 IC50 = 4.46 nM 8.35
CHEMBL4279929 IC50 = 5.24 nM 8.28
CHEMBL4287838 IC50 = 5.44 nM 8.26