Assay Detail
Binding
CHEMBL2424065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant human Trap-1 after 24 hrs by fluorescence polarization assay
10
Total Activities
10
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 |
Target
Heat shock protein 75 kDa, mitochondrial (CHEMBL1075132) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.12 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL252164 | LUMINESPIB | 2.0 | 1 | 7.42 |
| CHEMBL2103879 | GANETESPIB | 3.0 | 1 | 7.29 |
| CHEMBL467399 | BIIB021 | 2.0 | 1 | 7.05 |
| CHEMBL200102 | PU-H71 | 2.0 | 1 | 6.69 |
| CHEMBL278315 | GELDANAMYCIN | 2.0 | 1 | 6.18 |
| CHEMBL560895 | SNX-2112 | -1.0 | 1 | 6.14 |
| CHEMBL109480 | TANESPIMYCIN | 3.0 | 1 | 5.83 |
| CHEMBL2419346 | CUDC-305 | 1.0 | 1 | 5.80 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | 2.0 | 1 | 4.50 |
| CHEMBL14830 | ADENOSINE DIPHOSPHATE | 0.5 | 1 | 4.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL252164 | LUMINESPIB | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2103879 | GANETESPIB | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL467399 | BIIB021 | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL200102 | PU-H71 | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL278315 | GELDANAMYCIN | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL560895 | SNX-2112 | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL109480 | TANESPIMYCIN | IC50 | = | 1496.0 | nM | 5.83 |
| CHEMBL2419346 | CUDC-305 | IC50 | = | 1586.0 | nM | 5.80 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | IC50 | = | 31303.0 | nM | 4.50 |
| CHEMBL14830 | ADENOSINE DIPHOSPHATE | IC50 | = | 55594.0 | nM | 4.25 |