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Assay Detail

CHEMBL4627757

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

Binding
Displacement of [125I]MIP-1095 from PSMA in human PC3-PIP cells after 1 hr by gamma counter analysis
8
Total Activities
8
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

Synthesis and evaluation of novel radioiodinated PSMA targeting ligands for potential radiotherapy of prostate cancer.
Yao X, Zha Z, Ploessl K, Choi SR, Zhao R, Alexoff D, Zhu L, Kung HF.
Bioorg Med Chem (2020) 28 : 115319 -115319
PubMed 32001090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.41 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4636677 1 8.88
CHEMBL4636963 1 8.70
CHEMBL4649277 1 8.58
CHEMBL456029 MIP-1095 1.0 1 8.52
CHEMBL4639640 1 8.45
CHEMBL4648379 1 8.32
CHEMBL4594280 VIPIVOTIDE TETRAXETAN 2.0 1 7.96
CHEMBL4635514 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4636677 IC50 = 1.33 nM 8.88
CHEMBL4636963 IC50 = 1.99 nM 8.70
CHEMBL4649277 IC50 = 2.63 nM 8.58
CHEMBL456029 MIP-1095 IC50 = 3.0 nM 8.52
CHEMBL4639640 IC50 = 3.52 nM 8.45
CHEMBL4648379 IC50 = 4.74 nM 8.32
CHEMBL4594280 VIPIVOTIDE TETRAXETAN IC50 = 10.9 nM 7.96
CHEMBL4635514 IC50 = 13.0 nM 7.89