Assay Detail
Functional
CHEMBL4686982
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Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HL-60 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Hybrids of MEK inhibitor and NO donor as multitarget antitumor drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.78 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 8.89 |
| CHEMBL2103875 | TRAMETINIB | 4.0 | 1 | 8.52 |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | 8.22 |
| CHEMBL4791245 | — | — | 1 | 7.00 |
| CHEMBL4796522 | — | — | 1 | 6.85 |
| CHEMBL4740885 | — | — | 1 | 6.82 |
| CHEMBL4745039 | — | — | 1 | 6.60 |
| CHEMBL4776354 | — | — | 1 | 6.57 |
| CHEMBL4762919 | — | — | 1 | 6.54 |
| CHEMBL4741092 | — | — | 1 | 6.51 |
| CHEMBL4778955 | — | — | 1 | 6.41 |
| CHEMBL455983 | — | — | 1 | 6.28 |
| CHEMBL4791772 | — | — | 1 | 6.28 |
| CHEMBL4781475 | — | — | 1 | 6.26 |
| CHEMBL4792808 | — | — | 1 | 6.19 |
| CHEMBL4779702 | — | — | 1 | 6.11 |
| CHEMBL4779971 | — | — | 1 | 5.25 |
| CHEMBL4747266 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2103875 | TRAMETINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3264002 | AVUTOMETINIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4791245 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4796522 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4740885 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4745039 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4776354 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4762919 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4741092 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4778955 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL455983 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4791772 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4781475 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4792808 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4779702 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4779971 | — | IC50 | = | 5640.0 | nM | 5.25 |
| CHEMBL4747266 | — | IC50 | - | — | - |