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Assay Detail

CHEMBL998472

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Binding
Displacement of [3H]D-Asp from human EAAT1 receptor expressed in HEK293 cells
ChEMBL ↗
53
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Excitatory amino acid transporter 1 (CHEMBL3085) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1.
Jensen AA, Erichsen MN, Nielsen CW, Stensbøl TB, Kehler J, Bunch L.
J Med Chem (2009) 52 : 912 -915
PubMed 19161278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 5.12 6.18
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL474133 — — 2 6.18
CHEMBL473530 — — 2 5.68
CHEMBL451114 — — 2 5.64
CHEMBL462632 — — 2 5.57
CHEMBL474132 — — 2 5.50
CHEMBL515558 — — 2 5.44
CHEMBL461930 — — 2 5.44
CHEMBL516954 — — 2 5.40
CHEMBL515704 — — 2 5.37
CHEMBL512573 — — 2 5.33
CHEMBL517413 — — 2 5.33
CHEMBL474333 — — 2 5.14
CHEMBL473328 — — 2 5.13
CHEMBL474063 — — 2 5.04
CHEMBL504467 — — 2 5.00
CHEMBL516213 — — 2 4.97
CHEMBL460701 — — 2 4.85
CHEMBL516194 — — 2 4.52
CHEMBL474131 — — 2 4.52
CHEMBL460700 — — 2 4.30
CHEMBL321164 — — 1 4.00
CHEMBL28885 — — 1 4.00
CHEMBL472723 — — 2 4.00
CHEMBL473323 — — 2 -
CHEMBL473867 — — 2 -
CHEMBL474330 — — 2 -
CHEMBL475341 — — 1 -
CHEMBL514796 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL474133 — IC50 = 660.69 nM 6.18
CHEMBL474133 — IC50 = 660.0 nM 6.18
CHEMBL473530 — IC50 = 2100.0 nM 5.68
CHEMBL473530 — IC50 = 2137.96 nM 5.67
CHEMBL451114 — IC50 = 2290.87 nM 5.64
CHEMBL451114 — IC50 = 2300.0 nM 5.64
CHEMBL462632 — IC50 = 2700.0 nM 5.57
CHEMBL462632 — IC50 = 2754.23 nM 5.56
CHEMBL474132 — IC50 = 3200.0 nM 5.50
CHEMBL474132 — IC50 = 3235.94 nM 5.49
CHEMBL461930 — IC50 = 3630.78 nM 5.44
CHEMBL461930 — IC50 = 3600.0 nM 5.44
CHEMBL515558 — IC50 = 3600.0 nM 5.44
CHEMBL515558 — IC50 = 3630.78 nM 5.44
CHEMBL516954 — IC50 = 4000.0 nM 5.40
CHEMBL516954 — IC50 = 3981.07 nM 5.40
CHEMBL515704 — IC50 = 4265.8 nM 5.37
CHEMBL515704 — IC50 = 4300.0 nM 5.37
CHEMBL517413 — IC50 = 4700.0 nM 5.33
CHEMBL517413 — IC50 = 4677.35 nM 5.33
CHEMBL512573 — IC50 = 4700.0 nM 5.33
CHEMBL512573 — IC50 = 4786.3 nM 5.32
CHEMBL474333 — IC50 = 7300.0 nM 5.14
CHEMBL473328 — IC50 = 7400.0 nM 5.13
CHEMBL474333 — IC50 = 7413.1 nM 5.13
CHEMBL473328 — IC50 = 7413.1 nM 5.13
CHEMBL474063 — IC50 = 9200.0 nM 5.04
CHEMBL474063 — IC50 = 9120.11 nM 5.04
CHEMBL504467 — IC50 = 10000.0 nM 5.00
CHEMBL504467 — IC50 = 9900.0 nM 5.00
CHEMBL516213 — IC50 = 10715.19 nM 4.97
CHEMBL516213 — IC50 = 11000.0 nM 4.96
CHEMBL460701 — IC50 = 14125.38 nM 4.85
CHEMBL460701 — IC50 = 14000.0 nM 4.85
CHEMBL474131 — IC50 = 30000.0 nM 4.52
CHEMBL516194 — IC50 = 30000.0 nM 4.52
CHEMBL516194 — IC50 = 31622.78 nM 4.50
CHEMBL474131 — IC50 = 31622.78 nM 4.50
CHEMBL460700 — IC50 = 50118.72 nM 4.30
CHEMBL28885 — IC50 = 100000.0 nM 4.00
CHEMBL321164 — IC50 = 100000.0 nM 4.00
CHEMBL472723 — IC50 = 100000.0 nM 4.00
CHEMBL472723 — IC50 = 100000.0 nM 4.00
CHEMBL460700 — IC50 ~ 50000.0 nM -
CHEMBL473867 — IC50 > 316227.77 nM -
CHEMBL473867 — IC50 > 300000.0 nM -
CHEMBL474330 — IC50 > 316227.77 nM -
CHEMBL474330 — IC50 > 300000.0 nM -
CHEMBL514796 — IC50 > 316227.77 nM -
CHEMBL514796 — IC50 > 300000.0 nM -