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Assay Detail

CHEMBL2317558

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

Binding
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis
ChEMBL ↗
46
Total Activities
37
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

Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.
Sindelar M, Lutz TA, Petrera M, Wanner KT.
J Med Chem (2013) 56 : 1323 -1340
PubMed 23336362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.13 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473104 — — 2 7.40
CHEMBL1190520 — — 2 7.30
CHEMBL2315948 — — 1 7.21
CHEMBL1027 TIAGABINE 4.0 2 7.20
CHEMBL2315957 — — 2 7.10
CHEMBL2315958 — — 2 7.00
CHEMBL2315951 — — 1 6.90
CHEMBL38686 — — 2 6.90
CHEMBL2315997 — — 1 6.89
CHEMBL2315642 — — 1 6.59
CHEMBL2315952 — — 1 6.54
CHEMBL2315946 — — 1 6.32
CHEMBL2315995 — — 1 6.28
CHEMBL2315639 — — 1 6.11
CHEMBL2315944 — — 1 6.08
CHEMBL2315947 — — 1 6.01
CHEMBL2315641 — — 1 6.00
CHEMBL2315949 — — 1 5.91
CHEMBL2315998 — — 1 5.82
CHEMBL2315942 — — 1 5.81
CHEMBL2315643 — — 1 5.76
CHEMBL2315996 — — 1 5.75
CHEMBL2315950 — — 1 5.71
CHEMBL2315644 — — 1 5.65
CHEMBL2315945 — — 1 5.55
CHEMBL2315637 — — 1 5.55
CHEMBL2315623 — — 1 5.54
CHEMBL2315640 — — 1 5.48
CHEMBL2315635 — — 1 5.48
CHEMBL2315943 — — 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473104 — IC50 = 39.81 nM 7.40
CHEMBL473104 — IC50 = 40.0 nM 7.40
CHEMBL1190520 — IC50 = 50.12 nM 7.30
CHEMBL1190520 — IC50 = 55.0 nM 7.26
CHEMBL2315948 — IC50 = 61.24 nM 7.21
CHEMBL1027 TIAGABINE IC50 = 63.1 nM 7.20
CHEMBL1027 TIAGABINE IC50 = 70.0 nM 7.16
CHEMBL2315957 — IC50 = 80.0 nM 7.10
CHEMBL2315957 — IC50 = 79.43 nM 7.10
CHEMBL2315958 — IC50 = 100.0 nM 7.00
CHEMBL2315958 — IC50 = 111.0 nM 6.96
CHEMBL38686 — IC50 = 125.89 nM 6.90
CHEMBL2315951 — IC50 = 126.18 nM 6.90
CHEMBL38686 — IC50 = 130.0 nM 6.89
CHEMBL2315997 — IC50 = 128.53 nM 6.89
CHEMBL2315642 — IC50 = 254.68 nM 6.59
CHEMBL2315952 — IC50 = 291.74 nM 6.54
CHEMBL2315946 — IC50 = 478.63 nM 6.32
CHEMBL2315995 — IC50 = 528.45 nM 6.28
CHEMBL2315639 — IC50 = 769.13 nM 6.11
CHEMBL2315944 — IC50 = 835.6 nM 6.08
CHEMBL2315947 — IC50 = 972.75 nM 6.01
CHEMBL2315641 — IC50 = 997.7 nM 6.00
CHEMBL2315949 — IC50 = 1233.1 nM 5.91
CHEMBL2315998 — IC50 = 1499.68 nM 5.82
CHEMBL2315942 — IC50 = 1563.15 nM 5.81
CHEMBL2315643 — IC50 = 1725.84 nM 5.76
CHEMBL2315996 — IC50 = 1794.73 nM 5.75
CHEMBL2315950 — IC50 = 1958.84 nM 5.71
CHEMBL2315644 — IC50 = 2249.05 nM 5.65
CHEMBL2315945 — IC50 = 2824.88 nM 5.55
CHEMBL2315637 — IC50 = 2837.92 nM 5.55
CHEMBL2315623 — IC50 = 2870.78 nM 5.54
CHEMBL2315635 — IC50 = 3334.26 nM 5.48
CHEMBL2315640 — IC50 = 3318.94 nM 5.48
CHEMBL2315943 — IC50 = 3404.08 nM 5.47
CHEMBL2315636 — IC50 = 3564.51 nM 5.45
CHEMBL2315638 — IC50 = 3990.25 nM 5.40
CHEMBL2315994 — IC50 = 4920.4 nM 5.31
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 5011.87 nM 5.30
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 5000.0 nM 5.30
CHEMBL2315645 — IC50 = 7345.14 nM 5.13
CHEMBL277498 NIPECOTIC ACID IC50 = 7943.28 nM 5.10
CHEMBL277498 NIPECOTIC ACID IC50 = 8000.0 nM 5.10
CHEMBL76768 GUVACINE IC50 = 12589.25 nM 4.90
CHEMBL76768 GUVACINE IC50 = 14000.0 nM 4.85