Assay Detail
Binding
CHEMBL4021718
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Chaperone activity at FLAG/GFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as increase in localization of protein mutant in late endosomes after 24 hrs by Hoechst 33342 staining based fluorescence microscopic analysis
29
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
NPC intracellular cholesterol transporter 1 (CHEMBL1293277) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 5.12 | 6.82 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3311372 | — | — | 1 | 6.82 |
| CHEMBL4092121 | — | — | 1 | 5.44 |
| CHEMBL4076151 | — | — | 2 | 5.38 |
| CHEMBL3297906 | — | — | 1 | 4.96 |
| CHEMBL3298091 | — | — | 1 | 4.89 |
| CHEMBL4085267 | — | — | 1 | 4.85 |
| CHEMBL4075007 | — | — | 1 | 4.85 |
| CHEMBL4097145 | — | — | 1 | 4.80 |
| CHEMBL4070989 | — | — | 1 | 4.72 |
| CHEMBL4087738 | — | — | 1 | 4.52 |
| CHEMBL4070472 | — | — | 1 | - |
| CHEMBL4081569 | — | — | 1 | - |
| CHEMBL4091833 | — | — | 1 | - |
| CHEMBL4075527 | — | — | 1 | - |
| CHEMBL3297907 | — | — | 1 | - |
| CHEMBL3297908 | — | — | 1 | - |
| CHEMBL1091524 | — | — | 1 | - |
| CHEMBL1088982 | — | — | 1 | - |
| CHEMBL1088840 | — | — | 1 | - |
| CHEMBL1092220 | — | — | 1 | - |
| CHEMBL4079926 | — | — | 1 | - |
| CHEMBL4088731 | — | — | 1 | - |
| CHEMBL4069943 | — | — | 1 | - |
| CHEMBL4104163 | — | — | 1 | - |
| CHEMBL4098889 | — | — | 1 | - |
| CHEMBL4060496 | — | — | 1 | - |
| CHEMBL3297912 | — | — | 1 | - |
| CHEMBL4080856 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3311372 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4092121 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4076151 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3297906 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3298091 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4085267 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4075007 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4097145 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4070989 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4087738 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4070472 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL4081569 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL4091833 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4075527 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3297907 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL3297908 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL1091524 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL1088982 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL1088840 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL1092220 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4079926 | — | EC50 | - | — | - | |
| CHEMBL4088731 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4104163 | — | EC50 | - | — | - | |
| CHEMBL4076151 | — | Activity | - | — | - | |
| CHEMBL4098889 | — | EC50 | - | — | - | |
| CHEMBL4080856 | — | EC50 | - | — | - | |
| CHEMBL4069943 | — | EC50 | - | — | - | |
| CHEMBL3297912 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4060496 | — | EC50 | - | — | - |