Assay Detail
Binding
CHEMBL4433162
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosphatidylcholine as substrate after 1 hr by Amplex red fluorescence assay
14
Total Activities
14
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
Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.81 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453084 | — | — | 1 | 8.66 |
| CHEMBL4549771 | — | — | 1 | 8.60 |
| CHEMBL4476558 | — | — | 1 | 8.55 |
| CHEMBL4569141 | — | — | 1 | 8.40 |
| CHEMBL4454442 | — | — | 1 | 8.32 |
| CHEMBL3186509 | — | — | 1 | 8.08 |
| CHEMBL4462537 | — | — | 1 | 8.00 |
| CHEMBL4472840 | — | — | 1 | 7.70 |
| CHEMBL4446322 | — | — | 1 | 7.62 |
| CHEMBL4458386 | — | — | 1 | 7.28 |
| CHEMBL4561467 | — | — | 1 | 7.10 |
| CHEMBL4456849 | — | — | 1 | 6.91 |
| CHEMBL4588676 | — | — | 1 | 6.28 |
| CHEMBL4448598 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453084 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4549771 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4476558 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4569141 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4454442 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3186509 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4462537 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4472840 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4446322 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4458386 | — | IC50 | = | 52.3 | nM | 7.28 |
| CHEMBL4561467 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4456849 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4588676 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4448598 | — | IC50 | < | 1.7 | nM | - |