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Assay Detail

CHEMBL1034790

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Binding
Inhibition of [3H]glycine uptake at rat glycine transporter 2 expressed in african green monkey COS7 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Galanin receptor type 2 (CHEMBL5577)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New cyclic tetrapeptides from Nonomuraea sp. TA-0426 that inhibit glycine transporter type 1 (GlyT1).
Terui Y, Chu YW, Li JY, Ando T, Fukunaga T, Aoki T, Toda Y.
Bioorg Med Chem Lett (2008) 18 : 6321 -6323
PubMed 19013063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.56 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475562 1 7.68
CHEMBL451169 1 7.06
CHEMBL514318 1 6.65
CHEMBL515145 1 6.56
CHEMBL474037 1 6.35
CHEMBL474038 1 6.27
CHEMBL473840 1 6.24
CHEMBL475845 1 5.65
CHEMBL475216 1 -
CHEMBL180966 1 -
CHEMBL505699 1 -
CHEMBL443885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475562 IC50 = 21.1 nM 7.68
CHEMBL451169 IC50 = 87.7 nM 7.06
CHEMBL514318 IC50 = 226.0 nM 6.65
CHEMBL515145 IC50 = 278.0 nM 6.56
CHEMBL474037 IC50 = 450.0 nM 6.35
CHEMBL474038 IC50 = 542.0 nM 6.27
CHEMBL473840 IC50 = 574.0 nM 6.24
CHEMBL475845 IC50 = 2260.0 nM 5.65
CHEMBL475216 IC50 - -
CHEMBL180966 IC50 - -
CHEMBL505699 IC50 - -
CHEMBL443885 IC50 - -