Assay Detail
Binding
CHEMBL4682950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TDO assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 45 mins by microplate reader assay
75
Total Activities
75
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
Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 75 | 5.22 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4747079 | — | — | 1 | 7.60 |
| CHEMBL3989951 | NAVOXIMOD | 2.0 | 1 | 6.10 |
| CHEMBL4764324 | — | — | 1 | 5.84 |
| CHEMBL4763910 | — | — | 1 | 5.81 |
| CHEMBL4744944 | — | — | 1 | 5.77 |
| CHEMBL4779207 | — | — | 1 | 5.60 |
| CHEMBL4741917 | — | — | 1 | 5.60 |
| CHEMBL4762616 | — | — | 1 | 5.52 |
| CHEMBL4777678 | — | — | 1 | 5.46 |
| CHEMBL4763242 | — | — | 1 | 5.45 |
| CHEMBL4757365 | — | — | 1 | 5.44 |
| CHEMBL4755902 | — | — | 1 | 5.44 |
| CHEMBL4790626 | — | — | 1 | 5.39 |
| CHEMBL4764025 | — | — | 1 | 5.35 |
| CHEMBL4761417 | — | — | 1 | 5.29 |
| CHEMBL4793007 | — | — | 1 | 5.28 |
| CHEMBL4754740 | — | — | 1 | 5.28 |
| CHEMBL4786080 | — | — | 1 | 5.26 |
| CHEMBL4781631 | — | — | 1 | 5.26 |
| CHEMBL4759065 | — | — | 1 | 5.24 |
| CHEMBL4785586 | — | — | 1 | 5.19 |
| CHEMBL4784589 | — | — | 1 | 5.17 |
| CHEMBL4749277 | — | — | 1 | 5.15 |
| CHEMBL4752390 | — | — | 1 | 5.11 |
| CHEMBL4790494 | — | — | 1 | 5.07 |
| CHEMBL4746735 | — | — | 1 | 5.02 |
| CHEMBL4761665 | — | — | 1 | 4.98 |
| CHEMBL4761805 | — | — | 1 | 4.93 |
| CHEMBL4762872 | — | — | 1 | 4.78 |
| CHEMBL4762621 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4747079 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3989951 | NAVOXIMOD | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4764324 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL4763910 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4744944 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4779207 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL4741917 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL4762616 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL4777678 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL4763242 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL4757365 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL4755902 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL4790626 | — | IC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL4764025 | — | IC50 | = | 4460.0 | nM | 5.35 |
| CHEMBL4761417 | — | IC50 | = | 5130.0 | nM | 5.29 |
| CHEMBL4793007 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL4754740 | — | IC50 | = | 5240.0 | nM | 5.28 |
| CHEMBL4786080 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL4781631 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4759065 | — | IC50 | = | 5710.0 | nM | 5.24 |
| CHEMBL4785586 | — | IC50 | = | 6460.0 | nM | 5.19 |
| CHEMBL4784589 | — | IC50 | = | 6780.0 | nM | 5.17 |
| CHEMBL4749277 | — | IC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL4752390 | — | IC50 | = | 7690.0 | nM | 5.11 |
| CHEMBL4790494 | — | IC50 | = | 8480.0 | nM | 5.07 |
| CHEMBL4746735 | — | IC50 | = | 9630.0 | nM | 5.02 |
| CHEMBL4761665 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL4761805 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4762872 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL4762621 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL4749687 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL4790619 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL4791116 | — | IC50 | = | 23300.0 | nM | 4.63 |
| CHEMBL4793667 | — | IC50 | = | 31400.0 | nM | 4.50 |
| CHEMBL4753003 | — | IC50 | = | 41400.0 | nM | 4.38 |
| CHEMBL4743717 | — | IC50 | = | 46100.0 | nM | 4.34 |
| CHEMBL4750840 | — | IC50 | = | 99200.0 | nM | 4.00 |
| CHEMBL4744402 | — | IC50 | - | — | - | |
| CHEMBL4787467 | — | IC50 | - | — | - | |
| CHEMBL4754963 | — | IC50 | - | — | - | |
| CHEMBL4792447 | — | IC50 | - | — | - | |
| CHEMBL4789360 | — | IC50 | - | — | - | |
| CHEMBL4750827 | — | IC50 | - | — | - | |
| CHEMBL4758750 | — | IC50 | - | — | - | |
| CHEMBL4744959 | — | IC50 | - | — | - | |
| CHEMBL4752773 | — | IC50 | - | — | - | |
| CHEMBL4751368 | — | IC50 | - | — | - | |
| CHEMBL4749511 | — | IC50 | - | — | - | |
| CHEMBL4793321 | — | IC50 | - | — | - | |
| CHEMBL4789992 | — | IC50 | - | — | - |