Assay Detail
Binding
CHEMBL4252940
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FITC-geldanamycin binding to N-terminal domain of recombinant full-length HSP90alpha (unknown origin) after 16 hrs by fluorescence polarization assay
18
Total Activities
18
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
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.75 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4289811 | — | — | 1 | 8.28 |
| CHEMBL4279132 | — | — | 1 | 8.19 |
| CHEMBL4293186 | — | — | 1 | 7.94 |
| CHEMBL278315 | GELDANAMYCIN | 2.0 | 1 | 7.85 |
| CHEMBL4292004 | — | — | 1 | 6.87 |
| CHEMBL4280551 | — | — | 1 | 6.44 |
| CHEMBL4281389 | — | — | 1 | 6.38 |
| CHEMBL4291855 | — | — | 1 | 6.37 |
| CHEMBL4282602 | — | — | 1 | 6.34 |
| CHEMBL4294168 | — | — | 1 | 6.30 |
| CHEMBL4292279 | — | — | 1 | 6.28 |
| CHEMBL4285068 | — | — | 1 | 6.25 |
| CHEMBL4288435 | — | — | 1 | 6.23 |
| CHEMBL4283580 | — | — | 1 | 6.21 |
| CHEMBL4277126 | — | — | 1 | 6.08 |
| CHEMBL4281643 | — | — | 1 | 6.00 |
| CHEMBL4283995 | — | — | 1 | - |
| CHEMBL4278768 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4289811 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4279132 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4293186 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL278315 | GELDANAMYCIN | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4292004 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4280551 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL4281389 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL4291855 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL4282602 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4294168 | — | IC50 | = | 496.0 | nM | 6.30 |
| CHEMBL4292279 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL4285068 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL4288435 | — | IC50 | = | 585.0 | nM | 6.23 |
| CHEMBL4283580 | — | IC50 | = | 611.5 | nM | 6.21 |
| CHEMBL4277126 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4281643 | — | IC50 | = | 995.0 | nM | 6.00 |
| CHEMBL4283995 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4278768 | — | IC50 | > | 1000.0 | nM | - |