Assay Detail
Binding
CHEMBL4058731
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Inhibition of human recombinant IDO-1 using L-Trp as substrate after 15 mins by PDMAB-based assay
33
Total Activities
33
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
Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.53 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4061767 | — | — | 1 | 6.92 |
| CHEMBL4086143 | PF-06840003 | 1.0 | 1 | 6.82 |
| CHEMBL4077595 | — | — | 1 | 6.54 |
| CHEMBL4077425 | — | — | 1 | 6.43 |
| CHEMBL4076389 | — | — | 1 | 6.38 |
| CHEMBL4083811 | — | — | 1 | 6.31 |
| CHEMBL4075617 | — | — | 1 | 6.24 |
| CHEMBL4080809 | — | — | 1 | 6.21 |
| CHEMBL4071712 | — | — | 1 | 6.08 |
| CHEMBL4082296 | — | — | 1 | 5.92 |
| CHEMBL4071112 | — | — | 1 | 5.77 |
| CHEMBL4060549 | — | — | 1 | 5.77 |
| CHEMBL4087106 | — | — | 1 | 5.75 |
| CHEMBL4062070 | — | — | 1 | 5.75 |
| CHEMBL4068785 | — | — | 1 | 5.68 |
| CHEMBL4065315 | — | — | 1 | 5.66 |
| CHEMBL1374439 | — | — | 1 | 5.52 |
| CHEMBL4060093 | — | — | 1 | 5.47 |
| CHEMBL4089674 | — | — | 1 | 5.34 |
| CHEMBL4072559 | — | — | 1 | 5.10 |
| CHEMBL4073619 | — | — | 1 | 5.01 |
| CHEMBL4076482 | — | — | 1 | 4.75 |
| CHEMBL4094034 | — | — | 1 | 4.34 |
| CHEMBL4094955 | — | — | 1 | 4.28 |
| CHEMBL4065171 | — | — | 1 | 4.28 |
| CHEMBL4072984 | — | — | 1 | 4.27 |
| CHEMBL4090501 | — | — | 1 | 4.27 |
| CHEMBL4076509 | — | — | 1 | 4.08 |
| CHEMBL4099318 | — | — | 1 | - |
| CHEMBL4075749 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4061767 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4086143 | PF-06840003 | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4077595 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4077425 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4076389 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4083811 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4075617 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4080809 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4071712 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4082296 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4071112 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4060549 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4087106 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4062070 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4068785 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4065315 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1374439 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4060093 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4089674 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4072559 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4073619 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4076482 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4094034 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL4094955 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL4065171 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL4072984 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL4090501 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL4076509 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL4099318 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4075749 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4095166 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4098167 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4080434 | — | IC50 | > | 50000.0 | nM | - |