Assay Detail
Functional
CHEMBL5392287
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human A549 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
35
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Pharmacological Evaluation of Multisubstituted Pyrido[4,3-<i>d</i>]pyrimidine Analogues Bearing Deuterated Methylene Linkers as Potent KRAS<sup>G12D</sup> Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.95 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5417773 | — | — | 1 | 6.48 |
| CHEMBL5434863 | — | — | 1 | 6.30 |
| CHEMBL5428570 | — | — | 1 | 6.25 |
| CHEMBL5428592 | — | — | 1 | 6.16 |
| CHEMBL5398330 | — | — | 1 | 6.14 |
| CHEMBL5406625 | — | — | 1 | 6.03 |
| CHEMBL5425525 | — | — | 1 | 6.02 |
| CHEMBL5429420 | — | — | 1 | 6.02 |
| CHEMBL5401533 | — | — | 1 | 5.99 |
| CHEMBL5429156 | — | — | 1 | 5.96 |
| CHEMBL5398447 | — | — | 1 | 5.93 |
| CHEMBL5428081 | — | — | 1 | 5.77 |
| CHEMBL5402519 | — | — | 2 | 5.75 |
| CHEMBL5429942 | — | — | 1 | 5.67 |
| CHEMBL5407153 | — | — | 1 | 5.66 |
| CHEMBL5429727 | — | — | 1 | 5.65 |
| CHEMBL5429116 | — | — | 1 | 5.35 |
| CHEMBL5405563 | — | — | 1 | - |
| CHEMBL5415580 | — | — | 1 | - |
| CHEMBL5427525 | — | — | 1 | - |
| CHEMBL5400180 | — | — | 1 | - |
| CHEMBL5436886 | — | — | 1 | - |
| CHEMBL5421089 | — | — | 1 | - |
| CHEMBL5081048 | — | — | 1 | - |
| CHEMBL5412222 | — | — | 1 | - |
| CHEMBL5404424 | — | — | 1 | - |
| CHEMBL5415011 | — | — | 1 | - |
| CHEMBL5417307 | — | — | 1 | - |
| CHEMBL5434961 | — | — | 1 | - |
| CHEMBL5409510 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5417773 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL5434863 | — | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL5428570 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL5428592 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5398330 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL5406625 | — | IC50 | = | 944.0 | nM | 6.03 |
| CHEMBL5425525 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL5429420 | — | IC50 | = | 948.0 | nM | 6.02 |
| CHEMBL5401533 | — | IC50 | = | 1016.0 | nM | 5.99 |
| CHEMBL5429156 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL5398447 | — | IC50 | = | 1187.0 | nM | 5.93 |
| CHEMBL5428081 | — | IC50 | = | 1683.0 | nM | 5.77 |
| CHEMBL5402519 | — | IC50 | = | 1759.0 | nM | 5.75 |
| CHEMBL5429942 | — | IC50 | = | 2165.0 | nM | 5.67 |
| CHEMBL5407153 | — | IC50 | = | 2184.0 | nM | 5.66 |
| CHEMBL5429727 | — | IC50 | = | 2217.0 | nM | 5.65 |
| CHEMBL5429116 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5428093 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5402876 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5410913 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5402519 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5428596 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5409510 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5434961 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5417307 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5415011 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5404424 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5412222 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5405563 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5081048 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5421089 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5436886 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5415580 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5400180 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5427525 | — | IC50 | > | 5000.0 | nM | - |