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Assay Detail

CHEMBL1067317

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

Binding
Inhibition of human cloned glutamate carboxypeptidase 2
21
Total Activities
21
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

Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies.
Wang H, Byun Y, Barinka C, Pullambhatla M, Bhang HE, Fox JJ, Lubkowski J, Mease RC, Pomper MG.
Bioorg Med Chem Lett (2010) 20 : 392 -397
PubMed 19897367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.11 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596351 1 9.12
CHEMBL595408 1 8.28
CHEMBL604257 1 8.28
CHEMBL594123 1 7.96
CHEMBL593324 1 7.79
CHEMBL594262 1 7.79
CHEMBL593097 1 7.64
CHEMBL595441 1 7.62
CHEMBL595184 1 7.28
CHEMBL594019 1 7.07
CHEMBL595669 1 7.01
CHEMBL593331 1 6.98
CHEMBL594715 1 6.88
CHEMBL604488 1 6.59
CHEMBL593079 1 6.54
CHEMBL594267 1 6.50
CHEMBL593155 1 6.50
CHEMBL593090 1 6.10
CHEMBL593091 1 6.10
CHEMBL607543 1 5.88
CHEMBL608106 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596351 Ki = 0.75 nM 9.12
CHEMBL595408 Ki = 5.3 nM 8.28
CHEMBL604257 Ki = 5.3 nM 8.28
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
CHEMBL595441 Ki = 24.1 nM 7.62
CHEMBL595184 Ki = 52.3 nM 7.28
CHEMBL594019 Ki = 85.1 nM 7.07
CHEMBL595669 Ki = 97.2 nM 7.01
CHEMBL593331 Ki = 105.0 nM 6.98
CHEMBL594715 Ki = 132.0 nM 6.88
CHEMBL604488 Ki = 254.0 nM 6.59
CHEMBL593079 Ki = 285.0 nM 6.54
CHEMBL594267 Ki = 320.0 nM 6.50
CHEMBL593155 Ki = 318.0 nM 6.50
CHEMBL593090 Ki = 794.0 nM 6.10
CHEMBL593091 Ki = 795.0 nM 6.10
CHEMBL607543 Ki = 1320.0 nM 5.88
CHEMBL608106 Ki = 3430.0 nM 5.46