Assay Detail
ADMET
CHEMBL4020313
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Inhibition of human N-terminal 6His-tagged cytoplasmic LeuRS expressed in Escherichia coli BL21(DE3) assessed as L-[14C]leucine incorporation in to Escherichia coli tRNA after 20 mins by liquid scintillation counting analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.20 | 4.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077894 | — | — | 1 | 4.41 |
| CHEMBL4075879 | — | — | 1 | 4.17 |
| CHEMBL4105269 | — | — | 1 | 4.01 |
| CHEMBL4066786 | — | — | 1 | - |
| CHEMBL4086672 | — | — | 1 | - |
| CHEMBL4082159 | — | — | 1 | - |
| CHEMBL4081207 | — | — | 1 | - |
| CHEMBL4066833 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077894 | — | IC50 | = | 38800.0 | nM | 4.41 |
| CHEMBL4075879 | — | IC50 | = | 66900.0 | nM | 4.17 |
| CHEMBL4105269 | — | IC50 | = | 96600.0 | nM | 4.01 |
| CHEMBL4066786 | — | IC50 | = | 260000.0 | nM | - |
| CHEMBL4086672 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL4082159 | — | IC50 | = | 132000.0 | nM | - |
| CHEMBL4081207 | — | IC50 | = | 118000.0 | nM | - |
| CHEMBL4066833 | — | IC50 | = | 118000.0 | nM | - |