Assay Detail
Binding
CHEMBL5037986
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Inhibition of B0AT1 (unknown origin) by radiolabled uptake assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of novel, potent and orally efficacious inhibitor of neutral amino acid transporter B<sup>0</sup>AT1 (SLC6A19).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 6.10 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5082788 | — | — | 1 | 7.46 |
| CHEMBL5087496 | — | — | 1 | 7.05 |
| CHEMBL5094524 | — | — | 1 | 7.00 |
| CHEMBL5090717 | — | — | 1 | 6.82 |
| CHEMBL5077170 | — | — | 1 | 6.72 |
| CHEMBL5092865 | — | — | 1 | 6.70 |
| CHEMBL5083821 | — | — | 1 | 6.70 |
| CHEMBL5084448 | — | — | 1 | 6.50 |
| CHEMBL93233 | CINROMIDE | 2.0 | 1 | 6.43 |
| CHEMBL5092402 | — | — | 1 | 6.43 |
| CHEMBL5081155 | — | — | 1 | 6.36 |
| CHEMBL5075427 | — | — | 1 | 6.34 |
| CHEMBL5094851 | — | — | 1 | 6.28 |
| CHEMBL5092448 | — | — | 1 | 6.22 |
| CHEMBL5075355 | — | — | 1 | 6.22 |
| CHEMBL5074654 | — | — | 1 | 6.16 |
| CHEMBL5082943 | — | — | 1 | 6.10 |
| CHEMBL5085073 | — | — | 1 | 6.00 |
| CHEMBL5078017 | — | — | 1 | 6.00 |
| CHEMBL5078967 | — | — | 1 | 6.00 |
| CHEMBL5081254 | — | — | 1 | 5.41 |
| CHEMBL5088149 | — | — | 1 | 4.80 |
| CHEMBL56367 | NIMESULIDE | 4.0 | 1 | 4.64 |
| CHEMBL116590 | — | — | 1 | 4.15 |
| CHEMBL5085749 | — | — | 1 | 4.11 |
| CHEMBL5080716 | — | — | 1 | - |
| CHEMBL5090681 | — | — | 1 | - |
| CHEMBL5085836 | — | — | 1 | - |
| CHEMBL5092903 | — | — | 1 | - |
| CHEMBL5074840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5082788 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5087496 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5094524 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5090717 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5077170 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5092865 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5083821 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5084448 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL93233 | CINROMIDE | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5092402 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5081155 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5075427 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5094851 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5092448 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5075355 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5074654 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5082943 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5085073 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5078017 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5078967 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5081254 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5088149 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL56367 | NIMESULIDE | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL116590 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL5085749 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL5082944 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5094118 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5078865 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5074996 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5086886 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5078001 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5079561 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5086729 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5071501 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5094764 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5094598 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5077474 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5080716 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5085948 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5092919 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5083948 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5092819 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5092983 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5086307 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5074840 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5092903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5085836 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5090681 | — | IC50 | > | 10000.0 | nM | - |