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Assay Detail

CHEMBL1657779

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

Binding
Inhibition of [3H]glycine uptake at GlyT1 in rat C6 cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium- and chloride-dependent glycine transporter 1 (CHEMBL4556)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors.
Sugane T, Tobe T, Hamaguchi W, Shimada I, Maeno K, Miyata J, Suzuki T, Kimizuka T, Kohara A, Morita T, Doihara H, Saita K, Aota M, Furutani M, Shimada Y, Hamada N, Sakamoto S, Tsukamoto S.
J Med Chem (2011) 54 : 387 -391
PubMed 21141920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.78 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1649969 1 7.08
CHEMBL1649956 1 7.00
CHEMBL1649588 1 6.72
CHEMBL1649954 1 6.72
CHEMBL1649974 1 6.66
CHEMBL1649957 1 6.62
CHEMBL1649958 1 6.52
CHEMBL1649975 1 6.43
CHEMBL1649955 1 6.41
CHEMBL1649970 1 6.29
CHEMBL1649949 1 6.06
CHEMBL1649959 1 6.04
CHEMBL1649971 1 6.00
CHEMBL87351 1 5.75
CHEMBL1649968 1 5.64
CHEMBL1649976 1 5.58
CHEMBL1649952 1 5.52
CHEMBL1649960 1 5.42
CHEMBL1649950 1 5.28
CHEMBL1649972 1 5.19
CHEMBL1649964 1 5.01
CHEMBL1649961 1 4.96
CHEMBL1649967 1 4.57
CHEMBL1649951 1 4.46
CHEMBL1649965 1 4.21
CHEMBL1649966 1 4.16
CHEMBL1649963 1 -
CHEMBL1649962 1 -
CHEMBL1649953 1 -
CHEMBL1649973 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1649969 IC50 = 83.0 nM 7.08
CHEMBL1649956 IC50 = 100.0 nM 7.00
CHEMBL1649588 IC50 = 190.0 nM 6.72
CHEMBL1649954 IC50 = 190.0 nM 6.72
CHEMBL1649974 IC50 = 220.0 nM 6.66
CHEMBL1649957 IC50 = 240.0 nM 6.62
CHEMBL1649958 IC50 = 300.0 nM 6.52
CHEMBL1649975 IC50 = 370.0 nM 6.43
CHEMBL1649955 IC50 = 390.0 nM 6.41
CHEMBL1649970 IC50 = 510.0 nM 6.29
CHEMBL1649949 IC50 = 880.0 nM 6.06
CHEMBL1649959 IC50 = 920.0 nM 6.04
CHEMBL1649971 IC50 = 1000.0 nM 6.00
CHEMBL87351 IC50 = 1800.0 nM 5.75
CHEMBL1649968 IC50 = 2300.0 nM 5.64
CHEMBL1649976 IC50 = 2600.0 nM 5.58
CHEMBL1649952 IC50 = 3000.0 nM 5.52
CHEMBL1649960 IC50 = 3800.0 nM 5.42
CHEMBL1649950 IC50 = 5200.0 nM 5.28
CHEMBL1649972 IC50 = 6500.0 nM 5.19
CHEMBL1649964 IC50 = 9800.0 nM 5.01
CHEMBL1649961 IC50 = 11000.0 nM 4.96
CHEMBL1649967 IC50 = 27000.0 nM 4.57
CHEMBL1649951 IC50 = 35000.0 nM 4.46
CHEMBL1649965 IC50 = 62000.0 nM 4.21
CHEMBL1649966 IC50 = 70000.0 nM 4.16
CHEMBL1649963 IC50 > 100000.0 nM -
CHEMBL1649962 IC50 > 10000.0 nM -
CHEMBL1649953 IC50 > 30000.0 nM -
CHEMBL1649973 IC50 > 10000.0 nM -