Assay Detail
Functional
CHEMBL3132471
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Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum
46
Total Activities
46
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
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.71 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3125537 | — | — | 1 | 8.80 |
| CHEMBL3125697 | — | — | 1 | 8.60 |
| CHEMBL3125527 | — | — | 1 | 8.52 |
| CHEMBL3125698 | — | — | 1 | 8.47 |
| CHEMBL3125519 | — | — | 1 | 8.47 |
| CHEMBL3125700 | — | — | 1 | 8.47 |
| CHEMBL3125525 | — | — | 1 | 8.42 |
| CHEMBL3125701 | — | — | 1 | 8.40 |
| CHEMBL3125534 | — | — | 1 | 8.37 |
| CHEMBL3125521 | — | — | 1 | 8.36 |
| CHEMBL3125529 | — | — | 1 | 8.33 |
| CHEMBL3125538 | — | — | 1 | 8.32 |
| CHEMBL3125531 | — | — | 1 | 8.29 |
| CHEMBL3125517 | — | — | 1 | 8.28 |
| CHEMBL3125528 | — | — | 1 | 8.25 |
| CHEMBL3125524 | — | — | 1 | 8.24 |
| CHEMBL3125520 | — | — | 1 | 8.22 |
| CHEMBL3125526 | — | — | 1 | 8.22 |
| CHEMBL3125518 | — | — | 1 | 8.19 |
| CHEMBL3125535 | — | — | 1 | 8.15 |
| CHEMBL3125536 | — | — | 1 | 8.12 |
| CHEMBL3125533 | — | — | 1 | 8.09 |
| CHEMBL3125530 | — | — | 1 | 8.08 |
| CHEMBL3125540 | — | — | 1 | 8.06 |
| CHEMBL3125702 | NAVTEMADLIN | 3.0 | 1 | 8.04 |
| CHEMBL3125522 | — | — | 1 | 8.02 |
| CHEMBL3125539 | — | — | 1 | 7.85 |
| CHEMBL3125516 | — | — | 1 | 7.80 |
| CHEMBL3125532 | — | — | 1 | 7.70 |
| CHEMBL3125515 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3125537 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3125697 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3125527 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3125698 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3125519 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3125700 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3125525 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3125701 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3125534 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3125521 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3125529 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3125538 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3125531 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3125517 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3125528 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3125524 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3125520 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3125526 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3125518 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3125535 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3125536 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL3125533 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3125530 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3125540 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3125702 | NAVTEMADLIN | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3125522 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3125539 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3125516 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3125532 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3125515 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3125514 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3125513 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2402737 | IDASANUTLIN | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3125523 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2059435 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3125705 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3125699 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3125709 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3125706 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2381408 | SAR-405838 | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3125707 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3125710 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3125703 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2386346 | RO-5045337 | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL3125708 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3125704 | — | IC50 | = | 5500.0 | nM | 5.26 |