Assay Detail
Binding
CHEMBL4723504
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Inhibition of glycosylated human ATX using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured every 1 min for 30 mins by fluorescence microplate reader assay
34
Total Activities
34
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
Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.36 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744849 | — | — | 1 | 8.64 |
| CHEMBL3828074 | ZIRITAXESTAT | 3.0 | 1 | 8.51 |
| CHEMBL4787006 | — | — | 1 | 7.88 |
| CHEMBL4754625 | — | — | 1 | 7.00 |
| CHEMBL4776884 | — | — | 1 | 6.97 |
| CHEMBL4759554 | — | — | 1 | 6.96 |
| CHEMBL4759866 | — | — | 1 | 6.81 |
| CHEMBL4777413 | — | — | 1 | 6.72 |
| CHEMBL4800452 | — | — | 1 | 6.70 |
| CHEMBL4752284 | — | — | 1 | 6.63 |
| CHEMBL4782661 | — | — | 1 | 6.60 |
| CHEMBL4756394 | — | — | 1 | 6.55 |
| CHEMBL4752916 | — | — | 1 | 6.50 |
| CHEMBL4763503 | — | — | 1 | 6.46 |
| CHEMBL4759103 | — | — | 1 | 6.43 |
| CHEMBL4755901 | — | — | 1 | 6.39 |
| CHEMBL4756110 | — | — | 1 | 6.28 |
| CHEMBL4746859 | — | — | 1 | 6.23 |
| CHEMBL4788292 | — | — | 1 | 6.17 |
| CHEMBL4777851 | — | — | 1 | 6.15 |
| CHEMBL4636797 | — | — | 1 | 6.13 |
| CHEMBL4788354 | — | — | 1 | 6.09 |
| CHEMBL4759396 | — | — | 1 | 6.03 |
| CHEMBL4792046 | — | — | 1 | 5.89 |
| CHEMBL4784949 | — | — | 1 | 5.46 |
| CHEMBL4747364 | — | — | 1 | 5.39 |
| CHEMBL4756883 | — | — | 1 | 5.21 |
| CHEMBL4745581 | — | — | 1 | 5.20 |
| CHEMBL4744136 | — | — | 1 | 5.14 |
| CHEMBL4764462 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744849 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3828074 | ZIRITAXESTAT | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4787006 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL4754625 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4776884 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4759554 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4759866 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4777413 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4800452 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL4752284 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL4782661 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL4756394 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4752916 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4763503 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL4759103 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4755901 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4756110 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4746859 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4788292 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4777851 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4636797 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4788354 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4759396 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4792046 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4784949 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL4747364 | — | IC50 | = | 4050.0 | nM | 5.39 |
| CHEMBL4756883 | — | IC50 | = | 6140.0 | nM | 5.21 |
| CHEMBL4745581 | — | IC50 | = | 6370.0 | nM | 5.20 |
| CHEMBL4744136 | — | IC50 | = | 7240.0 | nM | 5.14 |
| CHEMBL4764462 | — | IC50 | = | 8270.0 | nM | 5.08 |
| CHEMBL4796166 | — | IC50 | = | 9230.0 | nM | 5.04 |
| CHEMBL4744993 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4749916 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4759532 | — | IC50 | > | 10000.0 | nM | - |