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Assay Detail

CHEMBL3579846

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

Binding
Inhibition of antiTEV-tagged GCP3 extracellular portion (aa 36-740) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
Tykvart J, Schimer J, Jančařík A, Bařinková J, Navrátil V, Starková J, Šrámková K, Konvalinka J, Majer P, Šácha P.
J Med Chem (2015) 58 : 4357 -4363
PubMed 25923815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.45 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510924 1 8.60
CHEMBL47009 1 8.57
CHEMBL3311268 1 8.09
CHEMBL3578202 GOZETOTIDE 4.0 1 7.89
CHEMBL3309678 1 7.85
CHEMBL3578201 1 7.80
CHEMBL3578197 1 7.00
CHEMBL596351 1 6.82
CHEMBL3578199 1 6.68
CHEMBL3578198 1 6.52
CHEMBL3578200 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510924 Ki = 2.5 nM 8.60
CHEMBL47009 Ki = 2.7 nM 8.57
CHEMBL3311268 Ki = 8.2 nM 8.09
CHEMBL3578202 GOZETOTIDE Ki = 13.0 nM 7.89
CHEMBL3309678 Ki = 14.0 nM 7.85
CHEMBL3578201 Ki = 16.0 nM 7.80
CHEMBL3578197 Ki = 100.0 nM 7.00
CHEMBL596351 Ki = 150.0 nM 6.82
CHEMBL3578199 Ki = 210.0 nM 6.68
CHEMBL3578198 Ki = 300.0 nM 6.52
CHEMBL3578200 Ki = 730.0 nM 6.14