Assay Detail
Functional
CHEMBL4481453
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs in presence of 100 uM octreotide followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay
19
Total Activities
19
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 | 19 | 6.32 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4575530 | — | — | 1 | 7.85 |
| CHEMBL4537192 | — | — | 1 | 6.94 |
| CHEMBL4534477 | — | — | 1 | 6.80 |
| CHEMBL4563111 | — | — | 1 | 6.70 |
| CHEMBL4550617 | — | — | 1 | 6.70 |
| CHEMBL4549303 | — | — | 1 | 6.66 |
| CHEMBL4532058 | — | — | 1 | 6.28 |
| CHEMBL4577466 | — | — | 1 | 6.25 |
| CHEMBL4581874 | — | — | 1 | 6.24 |
| CHEMBL4587303 | — | — | 1 | 6.19 |
| CHEMBL4592483 | — | — | 1 | 6.16 |
| CHEMBL4541310 | — | — | 1 | 6.12 |
| CHEMBL4556000 | — | — | 1 | 6.06 |
| CHEMBL4527856 | — | — | 1 | 6.04 |
| CHEMBL4584764 | — | — | 1 | 5.98 |
| CHEMBL4564727 | — | — | 1 | 5.86 |
| CHEMBL4581646 | — | — | 1 | 5.85 |
| CHEMBL4590517 | — | — | 1 | 5.80 |
| CHEMBL4548228 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4575530 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4537192 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4534477 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4563111 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4550617 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL4549303 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL4532058 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL4577466 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4581874 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL4587303 | — | IC50 | = | 644.0 | nM | 6.19 |
| CHEMBL4592483 | — | IC50 | = | 692.0 | nM | 6.16 |
| CHEMBL4541310 | — | IC50 | = | 757.0 | nM | 6.12 |
| CHEMBL4556000 | — | IC50 | = | 865.0 | nM | 6.06 |
| CHEMBL4527856 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4584764 | — | IC50 | = | 1041.0 | nM | 5.98 |
| CHEMBL4564727 | — | IC50 | = | 1389.0 | nM | 5.86 |
| CHEMBL4581646 | — | IC50 | = | 1427.0 | nM | 5.85 |
| CHEMBL4590517 | — | IC50 | = | 1597.0 | nM | 5.80 |
| CHEMBL4548228 | — | IC50 | = | 2524.0 | nM | 5.60 |