Assay Detail
Functional
CHEMBL4394493
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Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H727 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.24 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.60 |
| CHEMBL4451741 | — | — | 1 | 7.21 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 6.21 |
| CHEMBL4447840 | — | — | 1 | 6.16 |
| CHEMBL4449204 | — | — | 1 | 6.08 |
| CHEMBL64925 | MG-132 | — | 1 | 6.01 |
| CHEMBL4459808 | — | — | 1 | 5.35 |
| CHEMBL3319605 | — | — | 1 | 5.28 |
| CHEMBL374308 | LACTACYSTIN | — | 1 | - |
| CHEMBL4532449 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4451741 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 610.2 | nM | 6.21 |
| CHEMBL4447840 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4449204 | — | IC50 | = | 834.4 | nM | 6.08 |
| CHEMBL64925 | MG-132 | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4459808 | — | IC50 | = | 4490.0 | nM | 5.35 |
| CHEMBL3319605 | — | IC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL374308 | LACTACYSTIN | IC50 | > | 100000.0 | nM | - |
| CHEMBL4532449 | — | IC50 | > | 10000.0 | nM | - |