Assay Detail
Binding
CHEMBL3106549
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Binding affinity to human N-terminal polyHis-tagged GRP94 (L69 to N337) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay
6
Total Activities
6
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
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.96 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL252164 | LUMINESPIB | 2.0 | 1 | 8.40 |
| CHEMBL3104859 | — | — | 1 | 8.30 |
| CHEMBL467399 | BIIB021 | 2.0 | 1 | 6.75 |
| CHEMBL3104858 | — | — | 1 | 6.43 |
| CHEMBL560895 | SNX-2112 | -1.0 | 1 | 6.32 |
| CHEMBL3104860 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL252164 | LUMINESPIB | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3104859 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL467399 | BIIB021 | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL3104858 | — | Ki | = | 375.0 | nM | 6.43 |
| CHEMBL560895 | SNX-2112 | Ki | = | 484.0 | nM | 6.32 |
| CHEMBL3104860 | — | Ki | = | 2650.0 | nM | 5.58 |