Assay Detail
Functional
CHEMBL5611136
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H460 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of Novel Non-nucleoside DOT1L<sup>R231Q</sup> Inhibitors with Improved Pharmacokinetic Properties and Anti-lung Cancer Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 4.45 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5613348 | — | — | 1 | 5.54 |
| CHEMBL5612799 | — | — | 1 | 5.15 |
| CHEMBL5613873 | — | — | 1 | 5.02 |
| CHEMBL5613248 | — | — | 1 | 4.86 |
| CHEMBL5613146 | — | — | 1 | 4.84 |
| CHEMBL5612820 | — | — | 1 | 4.80 |
| CHEMBL5613382 | — | — | 1 | 4.79 |
| CHEMBL5612496 | — | — | 1 | 4.75 |
| CHEMBL5613349 | — | — | 1 | 4.66 |
| CHEMBL5614239 | — | — | 1 | 4.63 |
| CHEMBL5613244 | — | — | 1 | 4.59 |
| CHEMBL5612664 | — | — | 1 | 4.55 |
| CHEMBL5613936 | — | — | 1 | 4.53 |
| CHEMBL5613221 | — | — | 1 | 4.51 |
| CHEMBL5613646 | — | — | 1 | 4.45 |
| CHEMBL3087498 | — | — | 1 | 4.44 |
| CHEMBL5612738 | — | — | 1 | 4.44 |
| CHEMBL5614271 | — | — | 1 | 4.42 |
| CHEMBL5614286 | — | — | 1 | 4.42 |
| CHEMBL5613555 | — | — | 1 | 4.41 |
| CHEMBL5613104 | — | — | 1 | 4.39 |
| CHEMBL5612783 | — | — | 1 | 4.35 |
| CHEMBL5613652 | — | — | 1 | 4.34 |
| CHEMBL5613404 | — | — | 1 | 4.33 |
| CHEMBL5613809 | — | — | 1 | 4.32 |
| CHEMBL5612323 | — | — | 1 | 4.29 |
| CHEMBL5614032 | — | — | 1 | 4.28 |
| CHEMBL5612248 | — | — | 1 | 4.28 |
| CHEMBL5613370 | — | — | 1 | 4.19 |
| CHEMBL5614283 | — | — | 1 | 4.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5613348 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL5612799 | — | IC50 | = | 7150.0 | nM | 5.15 |
| CHEMBL5613873 | — | IC50 | = | 9590.0 | nM | 5.02 |
| CHEMBL5613248 | — | IC50 | = | 13850.0 | nM | 4.86 |
| CHEMBL5613146 | — | IC50 | = | 14490.0 | nM | 4.84 |
| CHEMBL5612820 | — | IC50 | = | 16010.0 | nM | 4.80 |
| CHEMBL5613382 | — | IC50 | = | 16230.0 | nM | 4.79 |
| CHEMBL5612496 | — | IC50 | = | 17610.0 | nM | 4.75 |
| CHEMBL5613349 | — | IC50 | = | 21840.0 | nM | 4.66 |
| CHEMBL5614239 | — | IC50 | = | 23190.0 | nM | 4.63 |
| CHEMBL5613244 | — | IC50 | = | 25600.0 | nM | 4.59 |
| CHEMBL5612664 | — | IC50 | = | 28390.0 | nM | 4.55 |
| CHEMBL5613936 | — | IC50 | = | 29560.0 | nM | 4.53 |
| CHEMBL5613221 | — | IC50 | = | 30900.0 | nM | 4.51 |
| CHEMBL5613646 | — | IC50 | = | 35720.0 | nM | 4.45 |
| CHEMBL3087498 | — | IC50 | = | 36010.0 | nM | 4.44 |
| CHEMBL5612738 | — | IC50 | = | 36470.0 | nM | 4.44 |
| CHEMBL5614271 | — | IC50 | = | 37740.0 | nM | 4.42 |
| CHEMBL5614286 | — | IC50 | = | 38440.0 | nM | 4.42 |
| CHEMBL5613555 | — | IC50 | = | 38690.0 | nM | 4.41 |
| CHEMBL5613104 | — | IC50 | = | 40580.0 | nM | 4.39 |
| CHEMBL5612783 | — | IC50 | = | 44940.0 | nM | 4.35 |
| CHEMBL5613652 | — | IC50 | = | 45310.0 | nM | 4.34 |
| CHEMBL5613404 | — | IC50 | = | 47140.0 | nM | 4.33 |
| CHEMBL5613809 | — | IC50 | = | 48110.0 | nM | 4.32 |
| CHEMBL5612323 | — | IC50 | = | 50780.0 | nM | 4.29 |
| CHEMBL5614032 | — | IC50 | = | 52590.0 | nM | 4.28 |
| CHEMBL5612248 | — | IC50 | = | 52030.0 | nM | 4.28 |
| CHEMBL5613370 | — | IC50 | = | 64290.0 | nM | 4.19 |
| CHEMBL5614283 | — | IC50 | = | 66470.0 | nM | 4.18 |
| CHEMBL5613363 | — | IC50 | = | 73070.0 | nM | 4.14 |
| CHEMBL5614195 | — | IC50 | = | 73800.0 | nM | 4.13 |
| CHEMBL5614251 | — | IC50 | = | 81250.0 | nM | 4.09 |
| CHEMBL5613145 | — | IC50 | = | 83870.0 | nM | 4.08 |
| CHEMBL5613626 | — | IC50 | = | 83180.0 | nM | 4.08 |
| CHEMBL5613534 | — | IC50 | = | 85500.0 | nM | 4.07 |
| CHEMBL5612464 | — | IC50 | = | 89600.0 | nM | 4.05 |
| CHEMBL5613242 | — | IC50 | = | 91240.0 | nM | 4.04 |
| CHEMBL5613748 | — | IC50 | = | 95480.0 | nM | 4.02 |
| CHEMBL5613975 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5612388 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5612371 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5612304 | — | IC50 | > | 100000.0 | nM | - |