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Assay Detail

CHEMBL903409

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

Binding
Inhibition of [3H]glycine uptake at human GlyT2 expressed in HEK293 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening.
Lowe J, Drozda S, Qian W, Peakman MC, Liu J, Gibbs J, Harms J, Schmidt C, Fisher K, Strick C, Schmidt A, Vanase M, Lebel L.
Bioorg Med Chem Lett (2007) 17 : 1675 -1678
PubMed 17257843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.53 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239601 1 7.50
CHEMBL239603 1 6.50
CHEMBL394236 1 6.42
CHEMBL239605 1 6.40
CHEMBL393168 1 6.28
CHEMBL392350 1 6.07
CHEMBL392586 1 -
CHEMBL393169 1 -
CHEMBL392770 1 -
CHEMBL239598 1 -
CHEMBL239596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239601 IC50 = 31.5 nM 7.50
CHEMBL239603 IC50 = 319.0 nM 6.50
CHEMBL394236 IC50 = 385.0 nM 6.42
CHEMBL239605 IC50 = 401.0 nM 6.40
CHEMBL393168 IC50 = 531.0 nM 6.28
CHEMBL392350 IC50 = 857.0 nM 6.07
CHEMBL392586 IC50 - -
CHEMBL393169 IC50 - -
CHEMBL392770 IC50 - -
CHEMBL239598 IC50 - -
CHEMBL239596 IC50 - -