Assay Detail
Binding
CHEMBL4149710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TDO2 assessed as decrease in conversion of L-tryptophan to N-formylkynurenine preincubated for 5 mins followed by 0.2 mM substrate addition measured after 15 mins by RapidFire mass spectrometry based fluorescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 30 | 6.07 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173485 | — | — | 1 | 7.55 |
| CHEMBL4165554 | — | — | 1 | 7.54 |
| CHEMBL4166415 | — | — | 1 | 6.85 |
| CHEMBL4162962 | — | — | 1 | 6.72 |
| CHEMBL4174655 | — | — | 1 | 6.57 |
| CHEMBL4168975 | — | — | 1 | 6.54 |
| CHEMBL4166624 | — | — | 1 | 6.47 |
| CHEMBL4170344 | — | — | 1 | 6.30 |
| CHEMBL4170773 | — | — | 1 | 6.24 |
| CHEMBL4166941 | — | — | 1 | 6.19 |
| CHEMBL4160126 | — | — | 1 | 6.08 |
| CHEMBL4176841 | — | — | 1 | 5.80 |
| CHEMBL4177244 | — | — | 1 | 5.80 |
| CHEMBL4165043 | — | — | 1 | 5.77 |
| CHEMBL4177147 | — | — | 1 | 5.64 |
| CHEMBL4162432 | — | — | 1 | 5.51 |
| CHEMBL4163495 | — | — | 1 | 5.36 |
| CHEMBL4159044 | — | — | 1 | 5.11 |
| CHEMBL4171214 | — | — | 1 | 4.75 |
| CHEMBL2431088 | — | — | 1 | 4.60 |
| CHEMBL4160459 | — | — | 1 | - |
| CHEMBL4162109 | — | — | 1 | - |
| CHEMBL4170040 | — | — | 1 | - |
| CHEMBL1391894 | — | — | 1 | - |
| CHEMBL4168565 | — | — | 1 | - |
| CHEMBL4167857 | — | — | 1 | - |
| CHEMBL4159938 | — | — | 1 | - |
| CHEMBL4168362 | — | — | 1 | - |
| CHEMBL4163311 | — | — | 1 | - |
| CHEMBL4172771 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173485 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4165554 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4166415 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4162962 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4174655 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4168975 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4166624 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4170344 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4170773 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4166941 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4160126 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4176841 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4177244 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4165043 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4177147 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4162432 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4163495 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4159044 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4171214 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2431088 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4160459 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4162109 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4170040 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL1391894 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4168565 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4167857 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4159938 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4168362 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4163311 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4172771 | — | IC50 | > | 25000.0 | nM | - |