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Assay Detail

CHEMBL3294690

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

Binding
Displacement of NO711 from mouse GAT1 expressed in HEK293 cells by LC-MS/MS analysis
27
Total Activities
27
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

Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.
Kowalczyk P, Sałat K, Höfner GC, Mucha M, Rapacz A, Podkowa A, Filipek B, Wanner KT, Kulig K.
Eur J Med Chem (2014) 83 : 256 -273
PubMed 24973660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 4.69 5.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3289578 1 5.04
CHEMBL3289580 1 4.98
CHEMBL3289568 1 4.96
CHEMBL3289575 1 4.96
CHEMBL3289576 1 4.95
CHEMBL3289574 1 4.90
CHEMBL3289573 1 4.81
CHEMBL3289577 1 4.80
CHEMBL3289566 1 4.79
CHEMBL3289588 1 4.78
CHEMBL3289579 1 4.78
CHEMBL3289295 1 4.76
CHEMBL3289571 1 4.75
CHEMBL3289572 1 4.67
CHEMBL3289570 1 4.67
CHEMBL3289567 1 4.64
CHEMBL3289581 1 4.62
CHEMBL3289582 1 4.60
CHEMBL3289585 1 4.59
CHEMBL75035 1 4.56
CHEMBL3289583 1 4.53
CHEMBL3289586 1 4.52
CHEMBL3289569 1 4.51
CHEMBL3289584 1 4.49
CHEMBL3289587 1 4.47
CHEMBL3289294 1 4.20
CHEMBL3289293 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3289578 Ki = 9120.11 nM 5.04
CHEMBL3289580 Ki = 10471.29 nM 4.98
CHEMBL3289568 Ki = 10964.78 nM 4.96
CHEMBL3289575 Ki = 10964.78 nM 4.96
CHEMBL3289576 Ki = 11220.18 nM 4.95
CHEMBL3289574 Ki = 12589.25 nM 4.90
CHEMBL3289573 Ki = 15488.17 nM 4.81
CHEMBL3289577 Ki = 15848.93 nM 4.80
CHEMBL3289566 Ki = 16218.1 nM 4.79
CHEMBL3289588 Ki = 16595.87 nM 4.78
CHEMBL3289579 Ki = 16595.87 nM 4.78
CHEMBL3289295 Ki = 17378.01 nM 4.76
CHEMBL3289571 Ki = 17782.79 nM 4.75
CHEMBL3289572 Ki = 21379.62 nM 4.67
CHEMBL3289570 Ki = 21379.62 nM 4.67
CHEMBL3289567 Ki = 22908.68 nM 4.64
CHEMBL3289581 Ki = 23988.33 nM 4.62
CHEMBL3289582 Ki = 25118.86 nM 4.60
CHEMBL3289585 Ki = 25703.96 nM 4.59
CHEMBL75035 Ki = 27542.29 nM 4.56
CHEMBL3289583 Ki = 29512.09 nM 4.53
CHEMBL3289586 Ki = 30199.52 nM 4.52
CHEMBL3289569 Ki = 30902.95 nM 4.51
CHEMBL3289584 Ki = 32359.37 nM 4.49
CHEMBL3289587 Ki = 33884.42 nM 4.47
CHEMBL3289294 Ki = 63095.73 nM 4.20
CHEMBL3289293 Ki = 66069.34 nM 4.18