Assay Detail
Binding
CHEMBL4388992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GRP78 (26 to 636 residues) (unknown origin) expressed in Escherichia coli BL21 DE3 cells pre-incubated for 10 mins before FITC-NRLLLTG fluorescent peptide addition in presence of 10 uM ADP followed by further incubation for 2 hrs by fluorescence polarization assay
2
Total Activities
2
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
Endoplasmic reticulum chaperone BiP (CHEMBL1781865) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A high throughput substrate binding assay reveals hexachlorophene as an inhibitor of the ER-resident HSP70 chaperone GRP78.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 5.57 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL470334 | — | — | 1 | 6.10 |
| CHEMBL496 | HEXACHLOROPHENE | 4.0 | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL470334 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL496 | HEXACHLOROPHENE | IC50 | = | 9100.0 | nM | 5.04 |