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Assay Detail

CHEMBL3405540

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Binding
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
ChEMBL ↗
125
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure activity relationship of selective GABA uptake inhibitors.
Vogensen SB, Jørgensen L, Madsen KK, Jurik A, Borkar N, Rosatelli E, Nielsen B, Ecker GF, Schousboe A, Clausen RP.
Bioorg Med Chem (2015) 23 : 2480 -2488
PubMed 25882526 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 125 4.59 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1027 TIAGABINE 4.0 1 6.10
CHEMBL3403594 — — 2 5.16
CHEMBL3403597 — — 2 5.01
CHEMBL1446457 — — 1 4.72
CHEMBL3403604 — — 2 4.36
CHEMBL3403598 — — 2 4.11
CHEMBL3403588 — — 2 4.08
CHEMBL3403586 — — 2 4.02
CHEMBL3403576 — — 2 -
CHEMBL3403561 — — 1 -
CHEMBL3403577 — — 2 -
CHEMBL3400184 — — 2 -
CHEMBL3403578 — — 2 -
CHEMBL75035 — — 1 -
CHEMBL3403565 — — 2 -
CHEMBL3403582 — — 2 -
CHEMBL3403564 — — 2 -
CHEMBL3403563 — — 2 -
CHEMBL3403562 — — 2 -
CHEMBL3403575 — — 2 -
CHEMBL3403574 — — 2 -
CHEMBL3403573 — — 2 -
CHEMBL3403572 — — 2 -
CHEMBL3403571 — — 2 -
CHEMBL3403570 — — 2 -
CHEMBL3403569 — — 2 -
CHEMBL3403568 — — 1 -
CHEMBL3403567 — — 2 -
CHEMBL2326025 — — 4 -
CHEMBL3403566 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1027 TIAGABINE IC50 = 800.0 nM 6.10
CHEMBL3403594 — IC50 = 6918.31 nM 5.16
CHEMBL3403594 — IC50 = 6990.0 nM 5.16
CHEMBL3403597 — IC50 = 9772.37 nM 5.01
CHEMBL3403597 — IC50 = 9700.0 nM 5.01
CHEMBL1446457 — IC50 = 19000.0 nM 4.72
CHEMBL3403604 — IC50 = 43651.58 nM 4.36
CHEMBL3403604 — IC50 = 43820.0 nM 4.36
CHEMBL3403598 — IC50 = 77624.71 nM 4.11
CHEMBL3403598 — IC50 = 77700.0 nM 4.11
CHEMBL3403588 — IC50 = 83000.0 nM 4.08
CHEMBL3403588 — IC50 = 83176.38 nM 4.08
CHEMBL3403586 — IC50 = 95499.26 nM 4.02
CHEMBL3403586 — IC50 = 95600.0 nM 4.02
CHEMBL3403563 — IC50 = 1819700.86 nM -
CHEMBL3403612 — IC50 = 5248074.6 nM -
CHEMBL3403564 — IC50 = 630957.34 nM -
CHEMBL3403565 — IC50 = 446683.59 nM -
CHEMBL2326025 — IC50 = 169824.37 nM -
CHEMBL2326025 — IC50 = 407380.28 nM -
CHEMBL3403567 — IC50 = 537031.8 nM -
CHEMBL3403569 — IC50 = 213796.21 nM -
CHEMBL3403595 — IC50 = 281838.29 nM -
CHEMBL3403583 — IC50 = 158489.32 nM -
CHEMBL445 NORTRIPTYLINE IC50 = 389045.14 nM -
CHEMBL3403585 — IC50 = 162181.01 nM -
CHEMBL3403587 — IC50 = 218776.16 nM -
CHEMBL3403590 — IC50 = 194984.46 nM -
CHEMBL3403593 — IC50 = 169824.37 nM -
CHEMBL3403608 — IC50 = 549540.87 nM -
CHEMBL3403607 — IC50 = 501187.23 nM -
CHEMBL3403605 — IC50 = 478630.09 nM -
CHEMBL2326030 — IC50 = 263026.8 nM -
CHEMBL3403576 — IC50 = 223872.11 nM -
CHEMBL3403556 — IC50 = 614000.0 nM -
CHEMBL3403556 — IC50 = 972000.0 nM -
CHEMBL3403555 — IC50 > 2000000.0 nM -
CHEMBL3403555 — IC50 > 2000000.0 nM -
CHEMBL3403554 — IC50 = 194000.0 nM -
CHEMBL2326030 — IC50 = 264000.0 nM -
CHEMBL75035 — IC50 > 30000.0 nM -
CHEMBL3403562 — IC50 = 1348962.88 nM -
CHEMBL3403554 — IC50 = 194984.46 nM -
CHEMBL3403556 — IC50 = 977237.22 nM -
CHEMBL3403556 — IC50 = 616595.0 nM -
CHEMBL3403557 — IC50 = 954992.59 nM -
CHEMBL3403558 — IC50 = 426579.52 nM -
CHEMBL3403558 — IC50 = 416869.38 nM -
CHEMBL3403559 — IC50 = 562341.33 nM -
CHEMBL2326022 — IC50 = 912010.84 nM -