Assay Detail
Binding
CHEMBL4836068
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Displacement of radio labeled-SIP from human recombinant S1P2 receptor expressed in CHO cell membranes measured after 15 mins by radioligand based competition binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.39 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4852127 | — | — | 1 | 6.72 |
| CHEMBL4860509 | — | — | 1 | 6.52 |
| CHEMBL4867313 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4852127 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4860509 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4867313 | — | IC50 | = | 1200.0 | nM | 5.92 |