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Assay Detail

CHEMBL680554

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Binding
Inhibition of human Glycine Transporter type-2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium- and chloride-dependent glycine transporter 2 (CHEMBL3060)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The first potent and selective inhibitors of the glycine transporter type 2.
Caulfield WL, Collie IT, Dickins RS, Epemolu O, McGuire R, Hill DR, McVey G, Morphy JR, Rankovic Z, Sundaram H.
J Med Chem (2001) 44 : 2679 -2682
PubMed 11495577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.32 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88588 1 7.80
CHEMBL431997 1 7.11
CHEMBL92310 1 7.08
CHEMBL88573 1 6.67
CHEMBL88800 1 6.25
CHEMBL91325 1 6.16
CHEMBL89493 1 5.88
CHEMBL90678 1 5.81
CHEMBL89571 1 5.64
CHEMBL89867 1 5.59
CHEMBL89866 1 5.55
CHEMBL91900 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88588 IC50 = 16.0 nM 7.80
CHEMBL431997 IC50 = 77.0 nM 7.11
CHEMBL92310 IC50 = 84.0 nM 7.08
CHEMBL88573 IC50 = 214.0 nM 6.67
CHEMBL88800 IC50 = 566.0 nM 6.25
CHEMBL91325 IC50 = 696.0 nM 6.16
CHEMBL89493 IC50 = 1321.0 nM 5.88
CHEMBL90678 IC50 = 1563.0 nM 5.81
CHEMBL89571 IC50 = 2313.0 nM 5.64
CHEMBL89867 IC50 = 2563.0 nM 5.59
CHEMBL89866 IC50 = 2816.0 nM 5.55
CHEMBL91900 IC50 > 10000.0 nM -