Assay Detail
Functional
CHEMBL4481444
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Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H524 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of an SSTR2-Targeting Maytansinoid Conjugate (PEN-221) with Potent Activity in Vitro and in Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.46 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201748 | CABAZITAXEL | 4.0 | 1 | 9.59 |
| CHEMBL2103835 | — | — | 1 | 8.43 |
| CHEMBL4575530 | — | — | 1 | 8.15 |
| CHEMBL4584764 | — | — | 1 | 8.10 |
| CHEMBL4527856 | — | — | 1 | 8.00 |
| CHEMBL4592483 | — | — | 1 | 8.00 |
| CHEMBL4563412 | — | — | 1 | 7.96 |
| CHEMBL4550617 | — | — | 1 | 7.82 |
| CHEMBL4541310 | — | — | 1 | 7.72 |
| CHEMBL4537192 | — | — | 1 | 7.66 |
| CHEMBL4581874 | — | — | 1 | 7.57 |
| CHEMBL4549303 | — | — | 1 | 7.52 |
| CHEMBL4564727 | — | — | 1 | 7.38 |
| CHEMBL4532058 | — | — | 1 | 7.36 |
| CHEMBL4556000 | — | — | 1 | 7.22 |
| CHEMBL4563111 | — | — | 1 | 7.12 |
| CHEMBL4548228 | — | — | 1 | 7.04 |
| CHEMBL4534477 | — | — | 1 | 6.82 |
| CHEMBL4590517 | — | — | 1 | 6.74 |
| CHEMBL4587303 | — | — | 1 | 6.24 |
| CHEMBL4581646 | — | — | 1 | 5.90 |
| CHEMBL4577466 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201748 | CABAZITAXEL | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2103835 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4575530 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4584764 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4527856 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4592483 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4563412 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4550617 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4541310 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4537192 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4581874 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4549303 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4564727 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4532058 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4556000 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4563111 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4548228 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4534477 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4590517 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4587303 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL4581646 | — | IC50 | = | 1258.0 | nM | 5.90 |
| CHEMBL4577466 | — | IC50 | = | 1473.0 | nM | 5.83 |