Assay Detail
Binding
CHEMBL4149709
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Inhibition of TDO2 in human SW48 cells assessed as decrease in conversion of tryptophan to N-formylkynurenine after 30 mins by fluorescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SW48 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.21 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166624 | — | — | 1 | 7.11 |
| CHEMBL4166415 | — | — | 1 | 7.07 |
| CHEMBL4173485 | — | — | 1 | 7.00 |
| CHEMBL4170773 | — | — | 1 | 6.68 |
| CHEMBL4168975 | — | — | 1 | 6.64 |
| CHEMBL4170344 | — | — | 1 | 6.60 |
| CHEMBL4177244 | — | — | 1 | 6.47 |
| CHEMBL4166941 | — | — | 1 | 6.44 |
| CHEMBL4162962 | — | — | 1 | 6.17 |
| CHEMBL4176841 | — | — | 1 | 6.09 |
| CHEMBL4165554 | — | — | 1 | 6.09 |
| CHEMBL4165043 | — | — | 1 | 6.09 |
| CHEMBL4160126 | — | — | 1 | 6.02 |
| CHEMBL4177147 | — | — | 1 | 5.85 |
| CHEMBL4162432 | — | — | 1 | 5.82 |
| CHEMBL4159044 | — | — | 1 | 5.82 |
| CHEMBL2431088 | — | — | 1 | 5.01 |
| CHEMBL4163495 | — | — | 1 | 4.75 |
| CHEMBL4174655 | — | — | 1 | - |
| CHEMBL4171214 | — | — | 1 | - |
| CHEMBL4163311 | — | — | 1 | - |
| CHEMBL4159938 | — | — | 1 | - |
| CHEMBL4167857 | — | — | 1 | - |
| CHEMBL4168565 | — | — | 1 | - |
| CHEMBL1391894 | — | — | 1 | - |
| CHEMBL4170040 | — | — | 1 | - |
| CHEMBL4162109 | — | — | 1 | - |
| CHEMBL4168362 | — | — | 1 | - |
| CHEMBL4160459 | — | — | 1 | - |
| CHEMBL4172771 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166624 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4166415 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4173485 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4170773 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4168975 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4170344 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4177244 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4166941 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4162962 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4176841 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4165554 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4165043 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4160126 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4177147 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4162432 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4159044 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2431088 | — | EC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4163495 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4174655 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4171214 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4163311 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4159938 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4167857 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4168565 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL1391894 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4170040 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4162109 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4168362 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4160459 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL4172771 | — | EC50 | > | 25000.0 | nM | - |