Assay Detail
Binding
CHEMBL5165218
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation activity against human ATX using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured every 30 mins by multi-mode microplate reader
25
Total Activities
25
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
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.30 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5177541 | — | — | 1 | 8.47 |
| CHEMBL3186509 | — | — | 1 | 8.43 |
| CHEMBL3828074 | ZIRITAXESTAT | 3.0 | 1 | 8.41 |
| CHEMBL5195787 | — | — | 1 | 8.15 |
| CHEMBL5189914 | — | — | 1 | 7.77 |
| CHEMBL5171446 | — | — | 1 | 7.62 |
| CHEMBL5189398 | — | — | 1 | 7.58 |
| CHEMBL5174427 | — | — | 1 | 7.47 |
| CHEMBL5171136 | — | — | 1 | 7.47 |
| CHEMBL5204000 | — | — | 1 | 7.39 |
| CHEMBL5194357 | — | — | 1 | 7.39 |
| CHEMBL5170680 | — | — | 1 | 7.29 |
| CHEMBL5192468 | — | — | 1 | 7.15 |
| CHEMBL5179219 | — | — | 1 | 7.09 |
| CHEMBL5190828 | — | — | 1 | 7.04 |
| CHEMBL5201210 | — | — | 1 | 6.89 |
| CHEMBL5200077 | — | — | 1 | 6.85 |
| CHEMBL5204526 | — | — | 1 | 6.81 |
| CHEMBL5189263 | — | — | 1 | 6.79 |
| CHEMBL5175013 | — | — | 1 | 6.77 |
| CHEMBL5179154 | — | — | 1 | 6.66 |
| CHEMBL5204769 | — | — | 1 | 6.63 |
| CHEMBL5200527 | — | — | 1 | 6.54 |
| CHEMBL5194595 | — | — | 1 | 6.50 |
| CHEMBL5208395 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5177541 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3186509 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3828074 | ZIRITAXESTAT | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5195787 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5189914 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5171446 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5189398 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL5174427 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5171136 | — | IC50 | = | 33.5 | nM | 7.47 |
| CHEMBL5204000 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5194357 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5170680 | — | IC50 | = | 51.3 | nM | 7.29 |
| CHEMBL5192468 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5179219 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5190828 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5201210 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL5200077 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5204526 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5189263 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL5175013 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5179154 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL5204769 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL5200527 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL5194595 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL5208395 | — | IC50 | > | 1000.0 | nM | - |