Assay Detail
Functional
CHEMBL4836071
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Antagonist activity at recombinant human S1P2 receptor in HFL1 cells assessed as inhibition of EC80 S1P-induced IL8 release incubated for 16 to 24 hrs in presence of 2% HSA by ELISA
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HFL1 |
| 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 | 14 | 4.33 | 4.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4877484 | — | — | 1 | 4.77 |
| CHEMBL4858923 | — | — | 1 | 4.50 |
| CHEMBL4871481 | — | — | 1 | 4.35 |
| CHEMBL4853790 | — | — | 1 | 4.31 |
| CHEMBL4847407 | — | — | 1 | 4.31 |
| CHEMBL4860157 | — | — | 1 | 4.17 |
| CHEMBL4861377 | — | — | 1 | 4.15 |
| CHEMBL4867946 | — | — | 1 | 4.06 |
| CHEMBL4878889 | — | — | 1 | - |
| CHEMBL4859853 | — | — | 1 | - |
| CHEMBL4856214 | — | — | 1 | - |
| CHEMBL4860408 | — | — | 1 | - |
| CHEMBL4866666 | — | — | 1 | - |
| CHEMBL4862597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4877484 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4858923 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4871481 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL4853790 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4847407 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4860157 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL4861377 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL4867946 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL4878889 | — | IC50 | = | 194000.0 | nM | - |
| CHEMBL4859853 | — | IC50 | = | 3220000.0 | nM | - |
| CHEMBL4856214 | — | IC50 | > | 10000000.0 | nM | - |
| CHEMBL4860408 | — | IC50 | = | 810000.0 | nM | - |
| CHEMBL4866666 | — | IC50 | = | 256000.0 | nM | - |
| CHEMBL4862597 | — | IC50 | > | 30000000.0 | nM | - |