Assay Detail
Binding
CHEMBL5347938
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ATX using LPC as substrate preincubated with compound for 15 mins followed by substrate addition measured after 30 mins by Amplex Red reagent based fluorescence analysis
33
Total Activities
33
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
"Hit" to lead optimization and chemoinformatic studies for a new series of Autotaxin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.06 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828074 | ZIRITAXESTAT | 3.0 | 1 | 6.70 |
| CHEMBL5434573 | — | — | 1 | 6.05 |
| CHEMBL5408703 | — | — | 1 | 5.70 |
| CHEMBL5402883 | — | — | 1 | 5.34 |
| CHEMBL5415947 | — | — | 1 | 5.28 |
| CHEMBL5408051 | — | — | 1 | 5.18 |
| CHEMBL5427479 | — | — | 1 | 5.17 |
| CHEMBL5422291 | — | — | 1 | 5.12 |
| CHEMBL5428151 | — | — | 1 | 4.95 |
| CHEMBL5439111 | — | — | 1 | 4.92 |
| CHEMBL5440421 | — | — | 1 | 4.80 |
| CHEMBL5396556 | — | — | 1 | 4.67 |
| CHEMBL5418211 | — | — | 1 | 4.61 |
| CHEMBL5427845 | — | — | 1 | 4.60 |
| CHEMBL5408393 | — | — | 1 | 4.43 |
| CHEMBL5425515 | — | — | 1 | 4.38 |
| CHEMBL5413441 | — | — | 1 | 4.16 |
| CHEMBL5401345 | — | — | 1 | - |
| CHEMBL5418016 | — | — | 1 | - |
| CHEMBL5410920 | — | — | 1 | - |
| CHEMBL5422275 | — | — | 1 | - |
| CHEMBL5405766 | — | — | 1 | - |
| CHEMBL5397676 | — | — | 1 | - |
| CHEMBL5438381 | — | — | 1 | - |
| CHEMBL5413900 | — | — | 1 | - |
| CHEMBL5432113 | — | — | 1 | - |
| CHEMBL5423018 | — | — | 1 | - |
| CHEMBL5412570 | — | — | 1 | - |
| CHEMBL5403453 | — | — | 1 | - |
| CHEMBL5404774 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828074 | ZIRITAXESTAT | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5434573 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5408703 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5402883 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5415947 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5408051 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5427479 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5422291 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL5428151 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL5439111 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL5440421 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5396556 | — | IC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL5418211 | — | IC50 | = | 24400.0 | nM | 4.61 |
| CHEMBL5427845 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5408393 | — | IC50 | = | 37300.0 | nM | 4.43 |
| CHEMBL5425515 | — | IC50 | = | 41800.0 | nM | 4.38 |
| CHEMBL5413441 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL5401345 | — | IC50 | - | — | - | |
| CHEMBL5418016 | — | IC50 | - | — | - | |
| CHEMBL5410920 | — | IC50 | - | — | - | |
| CHEMBL5422275 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5405766 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5397676 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5438381 | — | IC50 | - | — | - | |
| CHEMBL5413900 | — | IC50 | - | — | - | |
| CHEMBL5432113 | — | IC50 | - | — | - | |
| CHEMBL5423018 | — | IC50 | - | — | - | |
| CHEMBL5412570 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5403453 | — | IC50 | - | — | - | |
| CHEMBL5404774 | — | IC50 | - | — | - | |
| CHEMBL5432871 | — | IC50 | - | — | - | |
| CHEMBL5437000 | — | IC50 | - | — | - | |
| CHEMBL5414417 | — | IC50 | > | 100000.0 | nM | - |