Assay Detail
Binding
CHEMBL1048407
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Competitive inhibition of human autotaxin at free state isolated from MDA-MB-231 cells assessed as blockade of FS3 substrate hydrolysis by FRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Optimization of a pipemidic acid autotaxin inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.49 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL585744 | — | — | 1 | 6.16 |
| CHEMBL268789 | — | — | 1 | 5.72 |
| CHEMBL570590 | — | — | 1 | 5.40 |
| CHEMBL569652 | — | — | 1 | 5.38 |
| CHEMBL569873 | — | — | 1 | 5.35 |
| CHEMBL572167 | — | — | 1 | 5.24 |
| CHEMBL585743 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL585744 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL268789 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL570590 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL569652 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL569873 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL572167 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL585743 | — | Ki | = | 7100.0 | nM | 5.15 |