Assay Detail
Binding
CHEMBL970539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from human recombinant NPC1L1 expressed in HEK293 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
NPC1-like intracellular cholesterol transporter 1 (CHEMBL2027) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.69 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL504066 | — | — | 1 | 8.15 |
| CHEMBL321017 | — | — | 1 | 6.52 |
| CHEMBL466245 | — | — | 1 | 6.41 |
| CHEMBL466849 | — | — | 1 | 6.18 |
| CHEMBL468523 | — | — | 1 | 5.60 |
| CHEMBL513310 | — | — | 1 | 5.36 |
| CHEMBL468522 | — | — | 1 | 5.34 |
| CHEMBL506754 | — | — | 1 | 5.13 |
| CHEMBL506719 | — | — | 1 | 4.10 |
| CHEMBL466440 | — | — | 1 | 4.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL504066 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL321017 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL466245 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL466849 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL468523 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL513310 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL468522 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL506754 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL506719 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL466440 | — | IC50 | = | 81000.0 | nM | 4.09 |