Assay Detail
Binding
CHEMBL4824855
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Inhibition of wild type ERAP1 (unknown origin) using L-Rho-Succ-FKARKF as substrate preincubated for 15 mins followed by substrate addition and measured after 20 mins by flourescence assay
20
Total Activities
20
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 |
Target
Endoplasmic reticulum aminopeptidase 1 (CHEMBL5939) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of a Series of Benzofuran Selective ERAP1 Inhibitors: Biochemical and <i>In Silico</i> Studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.33 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4862557 | — | — | 1 | 7.47 |
| CHEMBL3416733 | — | — | 1 | 7.28 |
| CHEMBL4863142 | — | — | 1 | 7.00 |
| CHEMBL4875461 | — | — | 1 | 6.94 |
| CHEMBL4864508 | — | — | 1 | 6.92 |
| CHEMBL4855038 | — | — | 1 | 6.82 |
| CHEMBL4854530 | — | — | 1 | 6.58 |
| CHEMBL4847534 | — | — | 1 | 6.56 |
| CHEMBL4850551 | — | — | 1 | 6.42 |
| CHEMBL4854083 | — | — | 1 | 6.16 |
| CHEMBL4873254 | — | — | 1 | 5.99 |
| CHEMBL4853997 | — | — | 1 | 5.95 |
| CHEMBL4855147 | — | — | 1 | 5.79 |
| CHEMBL4852033 | — | — | 1 | 5.76 |
| CHEMBL4877678 | — | — | 1 | 5.75 |
| CHEMBL4849207 | — | — | 1 | 5.71 |
| CHEMBL4863578 | — | — | 1 | 5.57 |
| CHEMBL4846862 | — | — | 1 | 5.35 |
| CHEMBL4873293 | — | — | 1 | - |
| CHEMBL4858634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4862557 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3416733 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4863142 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4875461 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4864508 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4855038 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4854530 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL4847534 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4850551 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL4854083 | — | IC50 | = | 698.0 | nM | 6.16 |
| CHEMBL4873254 | — | IC50 | = | 1027.0 | nM | 5.99 |
| CHEMBL4853997 | — | IC50 | = | 1119.0 | nM | 5.95 |
| CHEMBL4855147 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL4852033 | — | IC50 | = | 1755.0 | nM | 5.76 |
| CHEMBL4877678 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL4849207 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL4863578 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL4846862 | — | IC50 | = | 4442.0 | nM | 5.35 |
| CHEMBL4873293 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4858634 | — | IC50 | > | 10000.0 | nM | - |