Assay Detail
Binding
CHEMBL4006066
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Inhibition of human ATX expressed in HEK293 Flp-In cells assessed as decrease in choline release from LPC measured every 30 secs for 90 mins by HVA based fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.32 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062929 | — | — | 1 | 7.70 |
| CHEMBL4093316 | — | — | 1 | 7.00 |
| CHEMBL4081367 | — | — | 1 | 6.89 |
| CHEMBL4105619 | — | — | 1 | 6.70 |
| CHEMBL4090866 | — | — | 1 | 6.68 |
| CHEMBL4071554 | — | — | 1 | 6.50 |
| CHEMBL4094214 | — | — | 1 | 6.30 |
| CHEMBL4070768 | — | — | 1 | 6.25 |
| CHEMBL4098586 | — | — | 1 | 6.14 |
| CHEMBL4085570 | — | — | 1 | 6.09 |
| CHEMBL4101049 | — | — | 1 | 6.00 |
| CHEMBL4083075 | — | — | 1 | 5.68 |
| CHEMBL4072603 | — | — | 1 | 5.60 |
| CHEMBL272427 | TAURURSODIOL | 4.0 | 1 | 4.99 |
| CHEMBL4064007 | — | — | 1 | - |
| CHEMBL4078911 | — | — | 1 | - |
| CHEMBL4096938 | — | — | 1 | - |
| CHEMBL4097881 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062929 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4093316 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4081367 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4105619 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4090866 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL4071554 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4094214 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4070768 | — | IC50 | = | 563.0 | nM | 6.25 |
| CHEMBL4098586 | — | IC50 | = | 717.0 | nM | 6.14 |
| CHEMBL4085570 | — | IC50 | = | 814.0 | nM | 6.09 |
| CHEMBL4101049 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4083075 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4072603 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL272427 | TAURURSODIOL | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL4064007 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4078911 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4096938 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4097881 | — | IC50 | > | 30000.0 | nM | - |