Assay Detail
Binding
CHEMBL4041760
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of fluorescein isothiocyanate labeled geldanamycin binding to recombinant Hsp90alpha (unknown origin) after 1 hr by fluorescence polarization assay
31
Total Activities
31
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 pharmacological evaluation of 4,5-diarylisoxazols bearing amino acid residues within the 3-amido motif as potent heat shock protein 90 (Hsp90) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.79 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072042 | — | — | 1 | 7.85 |
| CHEMBL4093385 | — | — | 1 | 7.68 |
| CHEMBL252164 | LUMINESPIB | 2.0 | 1 | 7.66 |
| CHEMBL4073419 | — | — | 1 | 7.55 |
| CHEMBL4096929 | — | — | 1 | 7.41 |
| CHEMBL4076195 | — | — | 1 | 7.14 |
| CHEMBL4105335 | — | — | 1 | 7.10 |
| CHEMBL4074892 | — | — | 1 | 7.01 |
| CHEMBL4095108 | — | — | 1 | 6.97 |
| CHEMBL4071863 | — | — | 1 | 6.95 |
| CHEMBL4092797 | — | — | 1 | 6.91 |
| CHEMBL4076047 | — | — | 1 | 6.82 |
| CHEMBL4082518 | — | — | 1 | 6.81 |
| CHEMBL4083722 | — | — | 1 | 6.72 |
| CHEMBL4105667 | — | — | 1 | 6.69 |
| CHEMBL4077202 | — | — | 1 | 6.69 |
| CHEMBL4101324 | — | — | 1 | 6.59 |
| CHEMBL4083380 | — | — | 1 | 6.58 |
| CHEMBL4077012 | — | — | 1 | 6.54 |
| CHEMBL4062362 | — | — | 1 | 6.51 |
| CHEMBL4077514 | — | — | 1 | 6.43 |
| CHEMBL4093400 | — | — | 1 | 6.40 |
| CHEMBL4098075 | — | — | 1 | 6.39 |
| CHEMBL4078145 | — | — | 1 | 6.37 |
| CHEMBL4090031 | — | — | 1 | 6.33 |
| CHEMBL4071988 | — | — | 1 | 6.29 |
| CHEMBL4063033 | — | — | 1 | 6.28 |
| CHEMBL4070995 | — | — | 1 | 6.13 |
| CHEMBL4078956 | — | — | 1 | 6.08 |
| CHEMBL4100533 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072042 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4093385 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL252164 | LUMINESPIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4073419 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4096929 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4076195 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4105335 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4074892 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4095108 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4071863 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4092797 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4076047 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4082518 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4083722 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4105667 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL4077202 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL4101324 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL4083380 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4077012 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4062362 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL4077514 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4093400 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL4098075 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL4078145 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL4090031 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL4071988 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL4063033 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL4070995 | — | IC50 | = | 749.0 | nM | 6.13 |
| CHEMBL4078956 | — | IC50 | = | 836.0 | nM | 6.08 |
| CHEMBL4100533 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4068951 | — | IC50 | > | 1000.0 | nM | - |