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Assay Detail

CHEMBL680555

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

Binding
Inhibitory activity against human glycine transporter type 2 (hGlyT2) expressed in Chinese hamster ovary (CHO) cell line
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors.
Ho KK, Appell KC, Baldwin JJ, Bohnstedt AC, Dong G, Guo T, Horlick R, Islam KR, Kultgen SG, Masterson CM, McDonald E, McMillan K, Morphy JR, Rankovic Z, Sundaram H, Webb M.
Bioorg Med Chem Lett (2004) 14 : 545 -548
PubMed 14698200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.49 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153717 1 7.62
CHEMBL153731 1 7.52
CHEMBL358473 1 7.48
CHEMBL155273 1 7.37
CHEMBL153630 1 7.25
CHEMBL150560 1 7.24
CHEMBL150377 1 7.17
CHEMBL348200 1 7.11
CHEMBL153075 1 7.09
CHEMBL153139 1 7.07
CHEMBL357936 1 7.05
CHEMBL153410 1 7.00
CHEMBL348211 1 6.92
CHEMBL149571 1 6.89
CHEMBL150901 1 6.89
CHEMBL150796 1 6.89
CHEMBL150954 1 6.85
CHEMBL153148 1 6.85
CHEMBL153331 1 6.77
CHEMBL433739 1 6.52
CHEMBL150522 1 6.50
CHEMBL153521 1 6.48
CHEMBL150505 1 6.43
CHEMBL150836 1 6.17
CHEMBL356187 1 5.96
CHEMBL153591 1 5.92
CHEMBL153154 1 5.92
CHEMBL2112891 1 5.85
CHEMBL150972 1 5.80
CHEMBL153680 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153717 IC50 = 24.0 nM 7.62
CHEMBL153731 IC50 = 30.0 nM 7.52
CHEMBL358473 IC50 = 33.0 nM 7.48
CHEMBL155273 IC50 = 43.0 nM 7.37
CHEMBL153630 IC50 = 56.0 nM 7.25
CHEMBL150560 IC50 = 58.0 nM 7.24
CHEMBL150377 IC50 = 67.0 nM 7.17
CHEMBL348200 IC50 = 77.0 nM 7.11
CHEMBL153075 IC50 = 81.0 nM 7.09
CHEMBL153139 IC50 = 86.0 nM 7.07
CHEMBL357936 IC50 = 89.0 nM 7.05
CHEMBL153410 IC50 = 99.0 nM 7.00
CHEMBL348211 IC50 = 120.0 nM 6.92
CHEMBL150796 IC50 = 130.0 nM 6.89
CHEMBL149571 IC50 = 130.0 nM 6.89
CHEMBL150901 IC50 = 130.0 nM 6.89
CHEMBL150954 IC50 = 140.0 nM 6.85
CHEMBL153148 IC50 = 140.0 nM 6.85
CHEMBL153331 IC50 = 170.0 nM 6.77
CHEMBL433739 IC50 = 300.0 nM 6.52
CHEMBL150522 IC50 = 320.0 nM 6.50
CHEMBL153521 IC50 = 330.0 nM 6.48
CHEMBL150505 IC50 = 370.0 nM 6.43
CHEMBL150836 IC50 = 670.0 nM 6.17
CHEMBL356187 IC50 = 1100.0 nM 5.96
CHEMBL153591 IC50 = 1200.0 nM 5.92
CHEMBL153154 IC50 = 1200.0 nM 5.92
CHEMBL2112891 IC50 = 1400.0 nM 5.85
CHEMBL150972 IC50 = 1600.0 nM 5.80
CHEMBL153680 IC50 = 1600.0 nM 5.80
CHEMBL152937 IC50 = 1800.0 nM 5.75
CHEMBL153296 IC50 = 1900.0 nM 5.72
CHEMBL150409 IC50 = 2400.0 nM 5.62
CHEMBL153355 IC50 = 3400.0 nM 5.47
CHEMBL152979 IC50 = 3400.0 nM 5.47
CHEMBL150502 IC50 = 4000.0 nM 5.40
CHEMBL421793 IC50 = 4100.0 nM 5.39
CHEMBL149515 IC50 = 4400.0 nM 5.36
CHEMBL150786 IC50 > 10000.0 nM -
CHEMBL153124 IC50 > 5000.0 nM -
CHEMBL151644 IC50 > 10000.0 nM -
CHEMBL153670 IC50 > 5000.0 nM -
CHEMBL348213 IC50 > 5000.0 nM -
CHEMBL153151 IC50 ~ 10000.0 nM -
CHEMBL150722 IC50 > 5000.0 nM -
CHEMBL155222 IC50 > 5000.0 nM -