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Assay Detail

CHEMBL2185174

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Binding
Binding affinity to NAALADase
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate carboxypeptidase 2 (CHEMBL1892)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer.
Graham K, Lesche R, Gromov AV, Böhnke N, Schäfer M, Hassfeld J, Dinkelborg L, Kettschau G.
J Med Chem (2012) 55 : 9510 -9520
PubMed 23025786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.89 11.00
IC50 1 6.73 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510924 1 11.00
CHEMBL189217 1 10.00
CHEMBL47009 1 9.52
CHEMBL604257 1 8.28
CHEMBL595408 1 8.28
CHEMBL46005 1 8.10
CHEMBL594123 1 7.96
CHEMBL593324 1 7.79
CHEMBL594262 1 7.79
CHEMBL593097 1 7.64
CHEMBL191467 1 7.52
CHEMBL334737 1 6.73
CHEMBL2177511 1 6.41
CHEMBL132183 1 6.16
CHEMBL2114987 1 5.96
CHEMBL2115435 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510924 Ki = 0.01 nM 11.00
CHEMBL189217 Ki = 0.1 nM 10.00
CHEMBL47009 Ki = 0.3 nM 9.52
CHEMBL604257 Ki = 5.3 nM 8.28
CHEMBL595408 Ki = 5.3 nM 8.28
CHEMBL46005 Ki = 8.0 nM 8.10
CHEMBL594123 Ki = 11.0 nM 7.96
CHEMBL593324 Ki = 16.1 nM 7.79
CHEMBL594262 Ki = 16.2 nM 7.79
CHEMBL593097 Ki = 23.0 nM 7.64
CHEMBL191467 Ki = 30.0 nM 7.52
CHEMBL334737 IC50 = 185.0 nM 6.73
CHEMBL2177511 Ki = 392.0 nM 6.41
CHEMBL132183 Ki = 700.0 nM 6.16
CHEMBL2114987 Ki = 1109.0 nM 5.96
CHEMBL2115435 Ki = 1285.0 nM 5.89