Assay Detail
Functional
CHEMBL3241173
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Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SJSA-1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.42 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3125537 | — | — | 1 | 8.70 |
| CHEMBL3125527 | — | — | 1 | 8.52 |
| CHEMBL3236361 | — | — | 1 | 8.48 |
| CHEMBL3236651 | — | — | 1 | 8.40 |
| CHEMBL3236653 | — | — | 1 | 8.40 |
| CHEMBL3236655 | — | — | 1 | 8.40 |
| CHEMBL3236356 | — | — | 1 | 8.30 |
| CHEMBL3236358 | — | — | 1 | 8.30 |
| CHEMBL3236642 | — | — | 1 | 8.22 |
| CHEMBL3236359 | — | — | 1 | 8.10 |
| CHEMBL3236649 | — | — | 1 | 8.10 |
| CHEMBL3236657 | — | — | 1 | 8.00 |
| CHEMBL3236648 | — | — | 1 | 7.96 |
| CHEMBL3236362 | — | — | 1 | 7.93 |
| CHEMBL3236665 | — | — | 1 | 7.92 |
| CHEMBL3236644 | — | — | 1 | 7.89 |
| CHEMBL3236635 | — | — | 1 | 7.82 |
| CHEMBL3236662 | — | — | 1 | 7.80 |
| CHEMBL3236357 | — | — | 1 | 7.80 |
| CHEMBL3236643 | — | — | 1 | 7.77 |
| CHEMBL3236647 | — | — | 1 | 7.75 |
| CHEMBL3236654 | — | — | 1 | 7.72 |
| CHEMBL3236659 | — | — | 1 | 7.66 |
| CHEMBL3236658 | — | — | 1 | 7.64 |
| CHEMBL3233049 | — | — | 1 | 7.64 |
| CHEMBL3236640 | — | — | 1 | 7.60 |
| CHEMBL3236636 | — | — | 1 | 7.57 |
| CHEMBL3236364 | — | — | 1 | 7.48 |
| CHEMBL3236660 | — | — | 1 | 7.44 |
| CHEMBL3233130 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3125537 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3125527 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3236361 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3236651 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3236653 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3236655 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3236356 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3236358 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3236642 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3236359 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3236649 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3236657 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3236648 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3236362 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL3236665 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3236644 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3236635 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3236662 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3236357 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3236643 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3236647 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3236654 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3236659 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3236658 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3233049 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3236640 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3236636 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3236364 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3236660 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3233130 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3236363 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2402737 | IDASANUTLIN | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3236639 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3236646 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3236663 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3236645 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3236661 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL3236652 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL2381408 | SAR-405838 | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3236664 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL3236656 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3236667 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3236666 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL3236637 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL3236650 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL3236365 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL2386346 | RO-5045337 | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL3236641 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3236360 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL3236638 | — | IC50 | = | 14500.0 | nM | 4.84 |