Assay Detail
Binding
CHEMBL904863
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Inhibition of human recombinant HSP90 in MCF7 cells assessed as Her2 degradation
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.31 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL109480 | TANESPIMYCIN | 3.0 | 1 | 8.15 |
| CHEMBL389164 | — | — | 1 | 8.05 |
| CHEMBL229943 | — | — | 1 | 7.82 |
| CHEMBL536072 | — | — | 1 | 7.70 |
| CHEMBL229577 | — | — | 1 | 7.57 |
| CHEMBL557165 | — | — | 1 | 7.52 |
| CHEMBL229891 | — | — | 1 | 7.46 |
| CHEMBL229576 | — | — | 1 | 7.38 |
| CHEMBL388549 | — | — | 1 | 7.30 |
| CHEMBL229691 | — | — | 1 | 7.26 |
| CHEMBL229690 | — | — | 1 | 7.16 |
| CHEMBL229839 | — | — | 1 | 7.10 |
| CHEMBL388347 | — | — | 1 | 7.05 |
| CHEMBL376166 | — | — | 1 | 7.05 |
| CHEMBL388550 | — | — | 1 | 6.47 |
| CHEMBL388821 | — | — | 1 | 6.16 |
| CHEMBL228406 | — | — | 1 | 6.00 |
| CHEMBL229838 | — | — | 1 | 5.82 |
| CHEMBL388134 | — | — | 1 | 5.82 |
| CHEMBL112953 | — | — | 1 | 5.77 |
| CHEMBL228990 | — | — | 1 | 5.75 |
| CHEMBL229639 | — | — | 1 | 5.70 |
| CHEMBL229638 | — | — | 1 | 5.52 |
| CHEMBL228407 | — | — | 1 | 5.24 |
| CHEMBL228989 | — | — | 1 | 5.12 |
| CHEMBL229692 | — | — | 1 | 4.77 |
| CHEMBL390557 | — | — | 1 | 4.35 |
| CHEMBL388822 | — | — | 1 | 4.30 |
| CHEMBL375462 | — | — | 1 | 4.00 |
| CHEMBL228991 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL109480 | TANESPIMYCIN | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL389164 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL229943 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL536072 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL229577 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL557165 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL229891 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL229576 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL388549 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL229691 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL229690 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL229839 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL388347 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL376166 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL388550 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL388821 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL228406 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL229838 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL388134 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL112953 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL228990 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL229639 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL229638 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL228407 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL228989 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL229692 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL390557 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL388822 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL375462 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL228991 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL229797 | — | IC50 | > | 10000.0 | nM | - |