Assay Detail
Binding
CHEMBL3865063
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Inhibition of ATX in human plasma assessed as decrease in hydrolysis of lysophosphatidylcholine by measuring choline release after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent inhibitors of the lysophospholipase autotaxin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.55 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3917975 | CAMBRITAXESTAT | 2.0 | 1 | 7.85 |
| CHEMBL3889955 | — | — | 1 | 7.80 |
| CHEMBL3917466 | — | — | 1 | 7.72 |
| CHEMBL3926932 | — | — | 1 | 7.58 |
| CHEMBL3982059 | — | — | 1 | 7.50 |
| CHEMBL3912114 | — | — | 1 | 7.47 |
| CHEMBL3946146 | — | — | 1 | 7.36 |
| CHEMBL3983022 | — | — | 1 | 7.00 |
| CHEMBL3964183 | — | — | 2 | 6.75 |
| CHEMBL3944813 | — | — | 1 | 6.67 |
| CHEMBL3916907 | — | — | 1 | 6.54 |
| CHEMBL3186509 | — | — | 1 | 6.54 |
| CHEMBL3907905 | — | — | 1 | 6.50 |
| CHEMBL3934551 | — | — | 1 | 6.48 |
| CHEMBL3907343 | — | — | 1 | 6.38 |
| CHEMBL3916898 | — | — | 1 | 6.35 |
| CHEMBL3954360 | — | — | 1 | 6.09 |
| CHEMBL3945659 | — | — | 1 | 5.98 |
| CHEMBL3899987 | — | — | 1 | 5.48 |
| CHEMBL3953575 | — | — | 1 | 5.24 |
| CHEMBL3935870 | — | — | 1 | 5.07 |
| CHEMBL1889181 | — | — | 1 | 5.05 |
| CHEMBL3965701 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3917975 | CAMBRITAXESTAT | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3889955 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3917466 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3926932 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3982059 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3912114 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3946146 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3983022 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3964183 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL3964183 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3944813 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL3186509 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL3916907 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL3907905 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL3934551 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL3907343 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL3916898 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL3954360 | — | IC50 | = | 821.0 | nM | 6.09 |
| CHEMBL3945659 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3899987 | — | IC50 | = | 3294.0 | nM | 5.48 |
| CHEMBL3953575 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3935870 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL1889181 | — | IC50 | = | 8870.0 | nM | 5.05 |
| CHEMBL3965701 | — | IC50 | = | 9700.0 | nM | 5.01 |