Assay Detail
Binding
CHEMBL4829376
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Inhibition of human 20S proteasome LMP2 using Ac-PAL-AMC as fluorogenic substrate measured every minute for 1 hr by fluorescence 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 |
Publication
Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.54 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4870740 | — | — | 1 | 7.18 |
| CHEMBL4867229 | — | — | 1 | 7.16 |
| CHEMBL4649310 | — | — | 1 | 7.15 |
| CHEMBL4646371 | — | — | 1 | 6.98 |
| CHEMBL4879354 | — | — | 1 | 6.89 |
| CHEMBL4845896 | — | — | 1 | 6.80 |
| CHEMBL4859824 | — | — | 1 | 6.80 |
| CHEMBL4875393 | — | — | 1 | 6.78 |
| CHEMBL4877277 | — | — | 1 | 6.74 |
| CHEMBL4869559 | — | — | 1 | 6.62 |
| CHEMBL4864020 | — | — | 1 | 6.60 |
| CHEMBL4866610 | — | — | 1 | 6.58 |
| CHEMBL4867231 | — | — | 1 | 6.38 |
| CHEMBL4863666 | — | — | 1 | 6.38 |
| CHEMBL4879280 | — | — | 1 | 6.37 |
| CHEMBL4863407 | — | — | 1 | 6.28 |
| CHEMBL4863075 | — | — | 1 | 6.25 |
| CHEMBL4849360 | — | — | 1 | 5.91 |
| CHEMBL4855585 | — | — | 1 | 5.67 |
| CHEMBL4854647 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4870740 | — | IC50 | = | 65.6 | nM | 7.18 |
| CHEMBL4867229 | — | IC50 | = | 69.4 | nM | 7.16 |
| CHEMBL4649310 | — | IC50 | = | 70.8 | nM | 7.15 |
| CHEMBL4646371 | — | IC50 | = | 105.2 | nM | 6.98 |
| CHEMBL4879354 | — | IC50 | = | 129.3 | nM | 6.89 |
| CHEMBL4845896 | — | IC50 | = | 157.9 | nM | 6.80 |
| CHEMBL4859824 | — | IC50 | = | 158.1 | nM | 6.80 |
| CHEMBL4875393 | — | IC50 | = | 167.7 | nM | 6.78 |
| CHEMBL4877277 | — | IC50 | = | 184.1 | nM | 6.74 |
| CHEMBL4869559 | — | IC50 | = | 237.7 | nM | 6.62 |
| CHEMBL4864020 | — | IC50 | = | 251.1 | nM | 6.60 |
| CHEMBL4866610 | — | IC50 | = | 261.5 | nM | 6.58 |
| CHEMBL4867231 | — | IC50 | = | 412.8 | nM | 6.38 |
| CHEMBL4863666 | — | IC50 | = | 414.5 | nM | 6.38 |
| CHEMBL4879280 | — | IC50 | = | 422.8 | nM | 6.37 |
| CHEMBL4863407 | — | IC50 | = | 522.6 | nM | 6.28 |
| CHEMBL4863075 | — | IC50 | = | 563.4 | nM | 6.25 |
| CHEMBL4849360 | — | IC50 | = | 1245.0 | nM | 5.91 |
| CHEMBL4855585 | — | IC50 | = | 2131.0 | nM | 5.67 |
| CHEMBL4854647 | — | IC50 | = | 4583.0 | nM | 5.34 |