Assay Detail
Binding
CHEMBL4143973
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Inhibition of recombinant rat ATX using LPC 18:1 as substrate after 2 hrs by rapidfire/MS-based analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.94 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4172309 | — | — | 1 | 8.89 |
| CHEMBL4173049 | — | — | 1 | 8.82 |
| CHEMBL4162641 | — | — | 1 | 8.77 |
| CHEMBL4168498 | — | — | 1 | 8.72 |
| CHEMBL4169550 | — | — | 1 | 8.64 |
| CHEMBL4173341 | — | — | 1 | 8.64 |
| CHEMBL4169912 | — | — | 1 | 8.51 |
| CHEMBL4165749 | BI 2545 | — | 1 | 8.47 |
| CHEMBL4170966 | — | — | 1 | 8.32 |
| CHEMBL4169136 | — | — | 1 | 8.26 |
| CHEMBL4164935 | — | — | 1 | 8.00 |
| CHEMBL4163050 | — | — | 1 | 7.86 |
| CHEMBL4159308 | — | — | 1 | 7.31 |
| CHEMBL4164658 | — | — | 1 | 7.17 |
| CHEMBL4174042 | — | — | 1 | 7.08 |
| CHEMBL4171105 | — | — | 1 | 5.82 |
| CHEMBL4162674 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4172309 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4173049 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4162641 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4168498 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4169550 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4173341 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4169912 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4165749 | BI 2545 | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4170966 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4169136 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4164935 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4163050 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4159308 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4164658 | — | IC50 | = | 66.9 | nM | 7.17 |
| CHEMBL4174042 | — | IC50 | = | 82.6 | nM | 7.08 |
| CHEMBL4171105 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4162674 | — | IC50 | = | 1674.0 | nM | 5.78 |