Assay Detail
Functional
CHEMBL834561
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Inhibitory concentration against NCI-H1299 cells was evaluated
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1299 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.26 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182319 | TALTOBULIN | 2.0 | 1 | 8.17 |
| CHEMBL188372 | — | — | 1 | 8.00 |
| CHEMBL181650 | — | — | 1 | 7.80 |
| CHEMBL188682 | — | — | 1 | 7.71 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 7.42 |
| CHEMBL189034 | — | — | 1 | 7.27 |
| CHEMBL454574 | — | — | 1 | 7.10 |
| CHEMBL186044 | — | — | 1 | 7.08 |
| CHEMBL186875 | — | — | 1 | 7.05 |
| CHEMBL185704 | — | — | 1 | 7.00 |
| CHEMBL362118 | — | — | 1 | 6.57 |
| CHEMBL425183 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182319 | TALTOBULIN | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL188372 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL181650 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL188682 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 37.7 | nM | 7.42 |
| CHEMBL189034 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL454574 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL186044 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL186875 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL185704 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL362118 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL425183 | — | IC50 | = | 1072.0 | nM | 5.97 |