Assay Detail
Binding
CHEMBL4771183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal His6-tagged ATX beta expressed in Sf9 insect cells using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured at 1 min interval for 30 mins by fluorescence assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.27 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4781471 | — | — | 1 | 8.68 |
| CHEMBL3828074 | ZIRITAXESTAT | 3.0 | 1 | 8.43 |
| CHEMBL3186509 | — | — | 1 | 8.37 |
| CHEMBL4797813 | — | — | 1 | 7.72 |
| CHEMBL4789880 | — | — | 1 | 7.24 |
| CHEMBL4783483 | — | — | 1 | 7.14 |
| CHEMBL4780733 | — | — | 1 | 6.98 |
| CHEMBL4800474 | — | — | 1 | 6.97 |
| CHEMBL4800586 | — | — | 1 | 6.94 |
| CHEMBL4778510 | — | — | 1 | 6.90 |
| CHEMBL4783759 | — | — | 1 | 6.80 |
| CHEMBL4789070 | — | — | 1 | 6.78 |
| CHEMBL4782735 | — | — | 1 | 6.70 |
| CHEMBL4789626 | — | — | 1 | 6.47 |
| CHEMBL4778972 | — | — | 1 | 6.25 |
| CHEMBL4797128 | — | — | 1 | 6.21 |
| CHEMBL4778764 | — | — | 1 | 6.11 |
| CHEMBL4788333 | — | — | 1 | 6.06 |
| CHEMBL4794345 | — | — | 1 | 6.04 |
| CHEMBL4780782 | — | — | 1 | 6.03 |
| CHEMBL4781407 | — | — | 1 | 6.01 |
| CHEMBL4798227 | — | — | 1 | 5.92 |
| CHEMBL4786557 | — | — | 1 | 5.90 |
| CHEMBL4800643 | — | — | 1 | 5.88 |
| CHEMBL4782134 | — | — | 1 | 5.85 |
| CHEMBL4779021 | — | — | 1 | 5.84 |
| CHEMBL4778551 | — | — | 1 | 5.81 |
| CHEMBL4794349 | — | — | 1 | 5.76 |
| CHEMBL4784566 | — | — | 1 | 5.73 |
| CHEMBL4776130 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4781471 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3828074 | ZIRITAXESTAT | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3186509 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4797813 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4789880 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4783483 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4780733 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4800474 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4800586 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4778510 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4783759 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4789070 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4782735 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL4789626 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL4778972 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4797128 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4778764 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4788333 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4794345 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4780782 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4781407 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4798227 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4786557 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4800643 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4782134 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4779021 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4778551 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL4794349 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL4784566 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4776130 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL4776428 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4776596 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL4786412 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL4798803 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL4783040 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL4789996 | — | IC50 | = | 2970.0 | nM | 5.53 |
| CHEMBL4788199 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL4791877 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL4789065 | — | IC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL4800384 | — | IC50 | = | 4210.0 | nM | 5.38 |
| CHEMBL4779619 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL4796956 | — | IC50 | = | 6070.0 | nM | 5.22 |
| CHEMBL4778480 | — | IC50 | > | 10000.0 | nM | - |