Assay Detail
Binding
CHEMBL4432509
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6x-His tagged human recombinant full length Hsp90alpha ATPase preincubated for 0.5 hrs followed by ATP addition measured after 30 mins by HTRF assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 4.66 | 6.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | 2.0 | 1 | 6.04 |
| CHEMBL4593194 | — | — | 1 | 5.43 |
| CHEMBL4564026 | — | — | 1 | 5.21 |
| CHEMBL4439457 | — | — | 1 | 5.07 |
| CHEMBL4515544 | — | — | 1 | 4.87 |
| CHEMBL4572319 | — | — | 1 | 4.84 |
| CHEMBL4450787 | — | — | 1 | 4.82 |
| CHEMBL1762708 | — | — | 1 | 4.81 |
| CHEMBL555017 | GAMBOGIC ACID | — | 1 | 4.66 |
| CHEMBL4452643 | — | — | 1 | 4.65 |
| CHEMBL4575582 | — | — | 1 | 4.64 |
| CHEMBL1762712 | — | — | 1 | 4.62 |
| CHEMBL4515685 | — | — | 1 | 4.56 |
| CHEMBL4552658 | — | — | 1 | 4.55 |
| CHEMBL4437572 | — | — | 1 | 4.45 |
| CHEMBL4580862 | — | — | 1 | 4.44 |
| CHEMBL4472575 | — | — | 1 | 4.37 |
| CHEMBL4578413 | — | — | 1 | 4.37 |
| CHEMBL4441422 | — | — | 1 | 4.28 |
| CHEMBL4446842 | — | — | 1 | 4.26 |
| CHEMBL4581935 | — | — | 1 | 4.17 |
| CHEMBL4538037 | — | — | 1 | 4.12 |
| CHEMBL4560082 | — | — | 1 | 4.05 |
| CHEMBL4443399 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | IC50 | = | 919.0 | nM | 6.04 |
| CHEMBL4593194 | — | IC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL4564026 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4439457 | — | IC50 | = | 8520.0 | nM | 5.07 |
| CHEMBL4515544 | — | IC50 | = | 13620.0 | nM | 4.87 |
| CHEMBL4572319 | — | IC50 | = | 14330.0 | nM | 4.84 |
| CHEMBL4450787 | — | IC50 | = | 15290.0 | nM | 4.82 |
| CHEMBL1762708 | — | IC50 | = | 15530.0 | nM | 4.81 |
| CHEMBL555017 | GAMBOGIC ACID | IC50 | = | 21980.0 | nM | 4.66 |
| CHEMBL4452643 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL4575582 | — | IC50 | = | 22630.0 | nM | 4.64 |
| CHEMBL1762712 | — | IC50 | = | 23930.0 | nM | 4.62 |
| CHEMBL4515685 | — | IC50 | = | 27340.0 | nM | 4.56 |
| CHEMBL4552658 | — | IC50 | = | 28030.0 | nM | 4.55 |
| CHEMBL4437572 | — | IC50 | = | 35240.0 | nM | 4.45 |
| CHEMBL4580862 | — | IC50 | = | 36620.0 | nM | 4.44 |
| CHEMBL4472575 | — | IC50 | = | 42980.0 | nM | 4.37 |
| CHEMBL4578413 | — | IC50 | = | 42410.0 | nM | 4.37 |
| CHEMBL4441422 | — | IC50 | = | 52670.0 | nM | 4.28 |
| CHEMBL4446842 | — | IC50 | = | 54680.0 | nM | 4.26 |
| CHEMBL4581935 | — | IC50 | = | 67060.0 | nM | 4.17 |
| CHEMBL4538037 | — | IC50 | = | 76810.0 | nM | 4.12 |
| CHEMBL4560082 | — | IC50 | = | 89830.0 | nM | 4.05 |
| CHEMBL4443399 | — | IC50 | > | 100000.0 | nM | - |