Assay Detail
Binding
CHEMBL3859629
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Inhibition of DPP1 in human U937 cells using Gly-Phe-AFC as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.53 | 8.80 |
| pIC50 | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936580 | — | — | 1 | 8.80 |
| CHEMBL3972563 | — | — | 1 | 8.50 |
| CHEMBL3900409 | BRENSOCATIB | 3.0 | 1 | 8.40 |
| CHEMBL3980602 | — | — | 1 | 8.30 |
| CHEMBL3891374 | — | — | 1 | 8.20 |
| CHEMBL3261926 | — | — | 1 | 8.10 |
| CHEMBL3960432 | — | — | 1 | 8.10 |
| CHEMBL3962926 | — | — | 1 | 7.90 |
| CHEMBL3926554 | — | — | 1 | 7.90 |
| CHEMBL3972158 | — | — | 1 | 7.80 |
| CHEMBL3917575 | — | — | 1 | 7.80 |
| CHEMBL3927609 | — | — | 1 | 7.50 |
| CHEMBL3970692 | — | — | 1 | 7.50 |
| CHEMBL3927522 | — | — | 1 | 7.40 |
| CHEMBL3929272 | — | — | 1 | 6.80 |
| CHEMBL3908639 | — | — | 1 | 6.70 |
| CHEMBL3899487 | — | — | 1 | 6.40 |
| CHEMBL3937199 | — | — | 1 | 6.30 |
| CHEMBL3919313 | — | — | 1 | 6.30 |
| CHEMBL3906771 | — | — | 1 | 5.90 |
| CHEMBL3947105 | — | — | 1 | - |
| CHEMBL3945475 | — | — | 1 | - |
| CHEMBL3901320 | — | — | 1 | - |
| CHEMBL3954197 | — | — | 1 | - |
| CHEMBL3899584 | — | — | 1 | - |
| CHEMBL3942969 | — | — | 1 | - |
| CHEMBL3910381 | — | — | 1 | - |
| CHEMBL3938314 | — | — | 1 | - |
| CHEMBL3966946 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936580 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL3972563 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL3900409 | BRENSOCATIB | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL3980602 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL3891374 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3261926 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3960432 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3962926 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3926554 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3972158 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3917575 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3927609 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3970692 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3927522 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3929272 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3908639 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3899487 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3937199 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3919313 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3906771 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3947105 | — | pIC50 | - | — | - | |
| CHEMBL3945475 | — | pIC50 | - | — | - | |
| CHEMBL3901320 | — | pIC50 | - | — | - | |
| CHEMBL3954197 | — | pIC50 | - | — | - | |
| CHEMBL3899584 | — | pIC50 | - | — | - | |
| CHEMBL3942969 | — | pIC50 | - | — | - | |
| CHEMBL3910381 | — | pIC50 | - | — | - | |
| CHEMBL3938314 | — | pIC50 | - | — | - | |
| CHEMBL3966946 | — | pIC50 | - | — | - |