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Assay Detail

CHEMBL5510484

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

Binding
Binding affinity to human recombinant GCPIII assessed as dissociation constant by fluorescence polarization assay
24
Total Activities
24
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

N-acetylated-alpha-linked acidic dipeptidase 2 (CHEMBL2609)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Glutamate Carboxypeptidase III Ligands to Compete the Uptake of [<sup>177</sup>Lu]Lu-PSMA-617 in Healthy Organs.
Müller M, Lucaroni L, Favalli N, Bassi G, Neri D, Cazzamalli S, Oehler S.
J Med Chem (2024) 67 : 8247 -8260
PubMed 38716576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 24 7.85 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5560474 1 8.77
CHEMBL5557579 1 8.37
CHEMBL5565532 1 8.35
CHEMBL5561626 1 8.32
CHEMBL5561704 1 8.20
CHEMBL5561251 1 8.19
CHEMBL5558611 1 8.15
CHEMBL5557217 1 7.92
CHEMBL5557349 1 7.85
CHEMBL5555029 1 7.82
CHEMBL5556760 1 7.64
CHEMBL5558512 1 7.62
CHEMBL5555028 1 7.52
CHEMBL5561889 1 7.06
CHEMBL5532072 1 6.97
CHEMBL5562614 1 6.77
CHEMBL5562592 1 -
CHEMBL5560002 1 -
CHEMBL5542221 1 -
CHEMBL5518058 1 -
CHEMBL5565084 1 -
CHEMBL5556963 1 -
CHEMBL5555147 1 -
CHEMBL5566819 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5560474 Kd = 1.7 nM 8.77
CHEMBL5557579 Kd = 4.3 nM 8.37
CHEMBL5565532 Kd = 4.5 nM 8.35
CHEMBL5561626 Kd = 4.8 nM 8.32
CHEMBL5561704 Kd = 6.3 nM 8.20
CHEMBL5561251 Kd = 6.4 nM 8.19
CHEMBL5558611 Kd = 7.0 nM 8.15
CHEMBL5557217 Kd = 12.0 nM 7.92
CHEMBL5557349 Kd = 14.0 nM 7.85
CHEMBL5555029 Kd = 15.0 nM 7.82
CHEMBL5556760 Kd = 23.0 nM 7.64
CHEMBL5558512 Kd = 24.0 nM 7.62
CHEMBL5555028 Kd = 30.0 nM 7.52
CHEMBL5561889 Kd = 87.0 nM 7.06
CHEMBL5532072 Kd = 106.0 nM 6.97
CHEMBL5562614 Kd = 169.0 nM 6.77
CHEMBL5562592 Kd > 500.0 nM -
CHEMBL5560002 Kd > 500.0 nM -
CHEMBL5542221 Kd > 500.0 nM -
CHEMBL5518058 Kd > 300.0 nM -
CHEMBL5565084 Kd > 300.0 nM -
CHEMBL5556963 Kd > 300.0 nM -
CHEMBL5555147 Kd > 500.0 nM -
CHEMBL5566819 Kd > 2600.0 nM -