Assay Detail
Binding
CHEMBL4051887
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Inhibition of human ATX using LPC (16:0) as substrate after 30 mins by horseradish peroxidase/choline oxidase coupled enzyme based spectrophotometric analysis
11
Total Activities
11
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
Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.89 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084282 | — | — | 1 | 7.58 |
| CHEMBL4061747 | — | — | 1 | 7.57 |
| CHEMBL4096364 | — | — | 1 | 7.22 |
| CHEMBL4075483 | — | — | 1 | 6.99 |
| CHEMBL4091174 | — | — | 1 | 6.99 |
| CHEMBL3828074 | ZIRITAXESTAT | 3.0 | 1 | 6.88 |
| CHEMBL4095546 | — | — | 1 | 6.72 |
| CHEMBL4063869 | — | — | 1 | 6.61 |
| CHEMBL4098810 | — | — | 1 | 6.56 |
| CHEMBL4064872 | — | — | 1 | 6.53 |
| CHEMBL4069420 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4084282 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4061747 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4096364 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4075483 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4091174 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL3828074 | ZIRITAXESTAT | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4095546 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4063869 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL4098810 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4064872 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL4069420 | — | IC50 | = | 811.0 | nM | 6.09 |