Assay Detail
Binding
CHEMBL3076582
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Inhibition of Rattus norvegicus (rat) brain gamma-amino butyrate aminotransferase using gamma-amino butyrate as substrate assessed as decrease in NADPH generation after 30 min by spectrophotometric analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
4-aminobutyrate aminotransferase, mitochondrial (CHEMBL3148) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
-Amino butyric acid analogs as novel potent GABA-AT inhibitors: molecular docking, synthesis, and biological evaluation
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.76 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2283229 | — | — | 1 | 7.14 |
| CHEMBL2283230 | — | — | 1 | 7.04 |
| CHEMBL2283231 | — | — | 1 | 6.96 |
| CHEMBL2283321 | — | — | 1 | 6.89 |
| CHEMBL2283322 | — | — | 1 | 6.85 |
| CHEMBL2283232 | — | — | 1 | 6.82 |
| CHEMBL2283323 | — | — | 1 | 6.70 |
| CHEMBL2283221 | — | — | 1 | 6.62 |
| CHEMBL2283208 | — | — | 1 | 6.55 |
| CHEMBL2283209 | — | — | 1 | 6.52 |
| CHEMBL2283222 | — | — | 1 | 6.50 |
| CHEMBL2283223 | — | — | 1 | 6.43 |
| CHEMBL2283224 | — | — | 1 | 6.34 |
| CHEMBL2283210 | — | — | 1 | 6.25 |
| CHEMBL2283225 | — | — | 1 | 5.92 |
| CHEMBL2283226 | — | — | 1 | 5.56 |
| CHEMBL2283227 | — | — | 1 | 5.30 |
| CHEMBL2283228 | — | — | 1 | 5.18 |
| CHEMBL2283211 | — | — | 1 | 5.00 |
| CHEMBL2283212 | — | — | 1 | 5.00 |
| CHEMBL2283213 | — | — | 1 | 4.81 |
| CHEMBL2283214 | — | — | 1 | 4.78 |
| CHEMBL2283215 | — | — | 1 | 4.68 |
| CHEMBL2283216 | — | — | 1 | 4.68 |
| CHEMBL2283217 | — | — | 1 | 4.63 |
| CHEMBL2283218 | — | — | 1 | 4.59 |
| CHEMBL2283219 | — | — | 1 | 4.52 |
| CHEMBL89598 | VIGABATRIN | 4.0 | 1 | 4.38 |
| CHEMBL2283220 | — | — | 1 | 4.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2283229 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2283230 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2283231 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2283321 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2283322 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2283232 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2283323 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2283221 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2283208 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2283209 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2283222 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2283223 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2283224 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2283210 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL2283225 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL2283226 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL2283227 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL2283228 | — | IC50 | = | 6540.0 | nM | 5.18 |
| CHEMBL2283211 | — | IC50 | = | 9950.0 | nM | 5.00 |
| CHEMBL2283212 | — | IC50 | = | 10020.0 | nM | 5.00 |
| CHEMBL2283213 | — | IC50 | = | 15530.0 | nM | 4.81 |
| CHEMBL2283214 | — | IC50 | = | 16780.0 | nM | 4.78 |
| CHEMBL2283215 | — | IC50 | = | 20760.0 | nM | 4.68 |
| CHEMBL2283216 | — | IC50 | = | 20820.0 | nM | 4.68 |
| CHEMBL2283217 | — | IC50 | = | 23480.0 | nM | 4.63 |
| CHEMBL2283218 | — | IC50 | = | 25940.0 | nM | 4.59 |
| CHEMBL2283219 | — | IC50 | = | 30120.0 | nM | 4.52 |
| CHEMBL89598 | VIGABATRIN | IC50 | = | 41210.0 | nM | 4.38 |
| CHEMBL2283220 | — | IC50 | = | 44060.0 | nM | 4.36 |