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Assay Detail

CHEMBL5253198

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

Binding
Binding affinity to PSMA in human LNCaP cells after 45 mins in presence of 68Ga-labeled PSMA-10 by gamma counting 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

Linker Modification Strategies To Control the Prostate-Specific Membrane Antigen (PSMA)-Targeting and Pharmacokinetic Properties of DOTA-Conjugated PSMA Inhibitors.
Benešová M, Bauder-Wüst U, Schäfer M, Klika KD, Mier W, Haberkorn U, Kopka K, Eder M.
J Med Chem (2016) 59 : 1761 -1775
PubMed 26878194 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.18 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5283285 1 9.30
CHEMBL5270513 1 9.28
CHEMBL5275438 1 8.74
CHEMBL5279851 1 8.71
CHEMBL4594280 VIPIVOTIDE TETRAXETAN 2.0 1 8.63
CHEMBL5279511 1 8.21
CHEMBL5287113 1 8.20
CHEMBL5268818 1 8.12
CHEMBL5268703 1 8.05
CHEMBL5284385 1 8.03
CHEMBL3578202 GOZETOTIDE 4.0 1 7.92
CHEMBL5282249 1 7.89
CHEMBL5289867 1 7.82
CHEMBL5267599 1 7.75
CHEMBL5281545 1 7.71
CHEMBL5272927 1 7.68
CHEMBL5269260 1 7.61
CHEMBL5274946 1 7.54
CHEMBL5279223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5283285 Ki = 0.5 nM 9.30
CHEMBL5270513 Ki = 0.53 nM 9.28
CHEMBL5275438 Ki = 1.81 nM 8.74
CHEMBL5279851 Ki = 1.97 nM 8.71
CHEMBL4594280 VIPIVOTIDE TETRAXETAN Ki = 2.34 nM 8.63
CHEMBL5279511 Ki = 6.19 nM 8.21
CHEMBL5287113 Ki = 6.31 nM 8.20
CHEMBL5268818 Ki = 7.51 nM 8.12
CHEMBL5268703 Ki = 8.86 nM 8.05
CHEMBL5284385 Ki = 9.33 nM 8.03
CHEMBL3578202 GOZETOTIDE Ki = 12.0 nM 7.92
CHEMBL5282249 Ki = 12.78 nM 7.89
CHEMBL5289867 Ki = 15.31 nM 7.82
CHEMBL5267599 Ki = 17.7 nM 7.75
CHEMBL5281545 Ki = 19.4 nM 7.71
CHEMBL5272927 Ki = 20.96 nM 7.68
CHEMBL5269260 Ki = 24.71 nM 7.61
CHEMBL5274946 Ki = 28.6 nM 7.54
CHEMBL5279223 Ki - -