Assay Detail
Binding
CHEMBL4824941
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PU-H71-FITC3 binding to recombinant N-terminal Grp94 (unknown origin) incubated for 2 hrs 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 and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.95 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200102 | PU-H71 | 2.0 | 1 | 6.88 |
| CHEMBL4869481 | — | — | 1 | 6.71 |
| CHEMBL4863672 | — | — | 1 | 6.50 |
| CHEMBL4068596 | — | — | 1 | 6.35 |
| CHEMBL4866705 | — | — | 1 | 6.31 |
| CHEMBL4850126 | — | — | 1 | 6.19 |
| CHEMBL4870087 | — | — | 1 | 6.09 |
| CHEMBL4860652 | — | — | 1 | 6.08 |
| CHEMBL4879021 | — | — | 1 | 6.01 |
| CHEMBL4876871 | — | — | 1 | 5.99 |
| CHEMBL4853988 | — | — | 1 | 5.97 |
| CHEMBL4863988 | — | — | 1 | 5.97 |
| CHEMBL4871630 | — | — | 1 | 5.90 |
| CHEMBL4866958 | — | — | 1 | 5.76 |
| CHEMBL4870579 | — | — | 1 | 5.75 |
| CHEMBL4864922 | — | — | 1 | 5.73 |
| CHEMBL4857569 | — | — | 1 | 5.73 |
| CHEMBL4854861 | — | — | 1 | 5.67 |
| CHEMBL4867384 | — | — | 1 | 5.50 |
| CHEMBL4846028 | — | — | 1 | 5.47 |
| CHEMBL4865186 | — | — | 1 | 5.46 |
| CHEMBL4859919 | — | — | 1 | 5.46 |
| CHEMBL4872173 | — | — | 1 | 5.42 |
| CHEMBL4866835 | — | — | 1 | - |
| CHEMBL4874124 | — | — | 1 | - |
| CHEMBL4870476 | — | — | 1 | - |
| CHEMBL4870963 | — | — | 1 | - |
| CHEMBL4853048 | — | — | 1 | - |
| CHEMBL4846176 | — | — | 1 | - |
| CHEMBL4864235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200102 | PU-H71 | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4869481 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4863672 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4068596 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL4866705 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL4850126 | — | IC50 | = | 649.0 | nM | 6.19 |
| CHEMBL4870087 | — | IC50 | = | 812.0 | nM | 6.09 |
| CHEMBL4860652 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4879021 | — | IC50 | = | 986.0 | nM | 6.01 |
| CHEMBL4876871 | — | IC50 | = | 1017.0 | nM | 5.99 |
| CHEMBL4853988 | — | IC50 | = | 1065.0 | nM | 5.97 |
| CHEMBL4863988 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4871630 | — | IC50 | = | 1259.0 | nM | 5.90 |
| CHEMBL4866958 | — | IC50 | = | 1725.0 | nM | 5.76 |
| CHEMBL4870579 | — | IC50 | = | 1787.0 | nM | 5.75 |
| CHEMBL4864922 | — | IC50 | = | 1881.0 | nM | 5.73 |
| CHEMBL4857569 | — | IC50 | = | 1867.0 | nM | 5.73 |
| CHEMBL4854861 | — | IC50 | = | 2129.0 | nM | 5.67 |
| CHEMBL4867384 | — | IC50 | = | 3193.0 | nM | 5.50 |
| CHEMBL4846028 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL4865186 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL4859919 | — | IC50 | = | 3444.0 | nM | 5.46 |
| CHEMBL4872173 | — | IC50 | = | 3756.0 | nM | 5.42 |
| CHEMBL4866835 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4874124 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4870476 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4870963 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4853048 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4846176 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4864235 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4876733 | — | IC50 | > | 5000.0 | nM | - |