Assay Detail
Functional
CHEMBL4686980
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Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| 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 | 22 | 5.91 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103875 | TRAMETINIB | 4.0 | 1 | 7.72 |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | 7.28 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 7.05 |
| CHEMBL455983 | — | — | 1 | 6.30 |
| CHEMBL4776354 | — | — | 1 | 6.21 |
| CHEMBL4743982 | — | — | 1 | 6.19 |
| CHEMBL4791772 | — | — | 1 | 6.17 |
| CHEMBL4741092 | — | — | 1 | 6.15 |
| CHEMBL4762919 | — | — | 1 | 6.14 |
| CHEMBL4792808 | — | — | 1 | 6.12 |
| CHEMBL4779971 | — | — | 1 | 6.00 |
| CHEMBL4781475 | — | — | 1 | 5.91 |
| CHEMBL4745811 | — | — | 1 | 5.56 |
| CHEMBL4791245 | — | — | 1 | 5.46 |
| CHEMBL4796522 | — | — | 1 | 5.29 |
| CHEMBL4746795 | — | — | 1 | 5.27 |
| CHEMBL4740885 | — | — | 1 | 5.24 |
| CHEMBL4745039 | — | — | 1 | 5.19 |
| CHEMBL4752434 | — | — | 1 | 5.13 |
| CHEMBL4779702 | — | — | 1 | 4.99 |
| CHEMBL4778955 | — | — | 1 | 4.81 |
| CHEMBL4747266 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103875 | TRAMETINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3264002 | AVUTOMETINIB | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL455983 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4776354 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4743982 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4791772 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4741092 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4762919 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4792808 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4779971 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4781475 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4745811 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4791245 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL4796522 | — | IC50 | = | 5090.0 | nM | 5.29 |
| CHEMBL4746795 | — | IC50 | = | 5340.0 | nM | 5.27 |
| CHEMBL4740885 | — | IC50 | = | 5790.0 | nM | 5.24 |
| CHEMBL4745039 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4752434 | — | IC50 | = | 7350.0 | nM | 5.13 |
| CHEMBL4779702 | — | IC50 | = | 10330.0 | nM | 4.99 |
| CHEMBL4778955 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL4747266 | — | IC50 | - | — | - |