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Assay Detail

CHEMBL1647445

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

Binding
Displacement of [3H]Tiagabine from human recombinant GAT1 expressed in HEK293 cells by equilibrium binding assay
ChEMBL ↗
52
Total Activities
52
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 Autocuration

Target

Sodium- and chloride-dependent GABA transporter 1 (CHEMBL1903) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.
Pizzi DA, Leslie CP, Di Fabio R, Seri C, Bernasconi G, Squaglia M, Carnevale G, Falchi A, Greco E, Mangiarini L, Negri M.
Bioorg Med Chem Lett (2011) 21 : 602 -605
PubMed 21134748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 52 6.97 7.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1641613 — — 1 7.83
CHEMBL1027 TIAGABINE 4.0 1 7.77
CHEMBL1642396 — — 1 7.74
CHEMBL1642400 — — 1 7.72
CHEMBL1642378 — — 1 7.69
CHEMBL1642397 — — 1 7.66
CHEMBL1642376 — — 1 7.54
CHEMBL1642379 — — 1 7.53
CHEMBL1642384 — — 1 7.47
CHEMBL1642395 — — 1 7.42
CHEMBL1642401 — — 1 7.41
CHEMBL1642375 — — 1 7.39
CHEMBL1642394 — — 1 7.38
CHEMBL1642388 — — 1 7.33
CHEMBL1642398 — — 1 7.28
CHEMBL1642399 — — 1 7.27
CHEMBL1642381 — — 1 7.25
CHEMBL1642382 — — 1 7.23
CHEMBL1642391 — — 1 7.21
CHEMBL1642374 — — 1 7.16
CHEMBL1642393 — — 1 7.15
CHEMBL77626 — — 1 7.14
CHEMBL1642386 — — 1 7.14
CHEMBL1642385 — — 1 7.11
CHEMBL1642387 — — 1 7.05
CHEMBL1642377 — — 1 7.03
CHEMBL1642367 — — 1 7.03
CHEMBL1642368 — — 1 6.99
CHEMBL1642402 — — 1 6.86
CHEMBL1642389 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1641613 — Ki = 14.79 nM 7.83
CHEMBL1027 TIAGABINE Ki = 16.98 nM 7.77
CHEMBL1642396 — Ki = 18.2 nM 7.74
CHEMBL1642400 — Ki = 19.05 nM 7.72
CHEMBL1642378 — Ki = 20.42 nM 7.69
CHEMBL1642397 — Ki = 21.88 nM 7.66
CHEMBL1642376 — Ki = 28.84 nM 7.54
CHEMBL1642379 — Ki = 29.51 nM 7.53
CHEMBL1642384 — Ki = 33.88 nM 7.47
CHEMBL1642395 — Ki = 38.02 nM 7.42
CHEMBL1642401 — Ki = 38.9 nM 7.41
CHEMBL1642375 — Ki = 40.74 nM 7.39
CHEMBL1642394 — Ki = 41.69 nM 7.38
CHEMBL1642388 — Ki = 46.77 nM 7.33
CHEMBL1642398 — Ki = 52.48 nM 7.28
CHEMBL1642399 — Ki = 53.7 nM 7.27
CHEMBL1642381 — Ki = 56.23 nM 7.25
CHEMBL1642382 — Ki = 58.88 nM 7.23
CHEMBL1642391 — Ki = 61.66 nM 7.21
CHEMBL1642374 — Ki = 69.18 nM 7.16
CHEMBL1642393 — Ki = 70.79 nM 7.15
CHEMBL77626 — Ki = 72.44 nM 7.14
CHEMBL1642386 — Ki = 72.44 nM 7.14
CHEMBL1642385 — Ki = 77.62 nM 7.11
CHEMBL1642387 — Ki = 89.13 nM 7.05
CHEMBL1642377 — Ki = 93.33 nM 7.03
CHEMBL1642367 — Ki = 93.33 nM 7.03
CHEMBL1642368 — Ki = 102.33 nM 6.99
CHEMBL1642402 — Ki = 138.04 nM 6.86
CHEMBL1642389 — Ki = 158.49 nM 6.80
CHEMBL1642364 — Ki = 165.96 nM 6.78
CHEMBL1642365 — Ki = 199.53 nM 6.70
CHEMBL1642383 — Ki = 331.13 nM 6.48
CHEMBL1642390 — Ki = 354.81 nM 6.45
CHEMBL1642363 — Ki = 371.54 nM 6.43
CHEMBL1642370 — Ki = 371.54 nM 6.43
CHEMBL1642392 — Ki = 380.19 nM 6.42
CHEMBL1642373 — Ki = 380.19 nM 6.42
CHEMBL1642371 — Ki = 645.65 nM 6.19
CHEMBL1642369 — Ki = 676.08 nM 6.17
CHEMBL1642372 — Ki = 691.83 nM 6.16
CHEMBL1642403 — Ki = 831.76 nM 6.08
CHEMBL1642380 — Ki = 1071.52 nM 5.97
CHEMBL1642366 — Ki = 1905.46 nM 5.72
CHEMBL1642404 — Ki = 2754.23 nM 5.56
CHEMBL1642405 — Ki > 10000.0 nM -
CHEMBL1642406 — Ki > 10000.0 nM -
CHEMBL1642407 — Ki > 10000.0 nM -
CHEMBL1642408 — Ki > 10000.0 nM -
CHEMBL1642409 — Ki > 10000.0 nM -