Assay Detail
Functional
CHEMBL4836069
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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 absence of HSA by ELISA
26
Total Activities
26
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 | 26 | 7.90 | 10.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874736 | — | — | 1 | 10.49 |
| CHEMBL4864274 | — | — | 1 | 9.52 |
| CHEMBL4877932 | — | — | 1 | 9.37 |
| CHEMBL4850513 | — | — | 1 | 9.21 |
| CHEMBL4847056 | — | — | 1 | 9.11 |
| CHEMBL4874151 | — | — | 1 | 8.89 |
| CHEMBL4868016 | — | — | 1 | 8.65 |
| CHEMBL4858923 | — | — | 1 | 7.82 |
| CHEMBL4853790 | — | — | 1 | 7.80 |
| CHEMBL4871481 | — | — | 1 | 7.70 |
| CHEMBL4845783 | — | — | 1 | 7.66 |
| CHEMBL4877484 | — | — | 1 | 7.62 |
| CHEMBL4847407 | — | — | 1 | 7.58 |
| CHEMBL4867946 | — | — | 1 | 7.54 |
| CHEMBL4860157 | — | — | 1 | 7.46 |
| CHEMBL4861377 | — | — | 1 | 7.44 |
| CHEMBL4869752 | — | — | 1 | 7.26 |
| CHEMBL4858509 | — | — | 1 | 6.98 |
| CHEMBL4866666 | — | — | 1 | 6.80 |
| CHEMBL4878889 | — | — | 1 | 6.62 |
| CHEMBL4859853 | — | — | 1 | 6.19 |
| CHEMBL4860408 | — | — | 1 | 6.15 |
| CHEMBL4846795 | — | — | 1 | - |
| CHEMBL4856214 | — | — | 1 | - |
| CHEMBL4847413 | — | — | 1 | - |
| CHEMBL4862597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874736 | — | IC50 | = | 0.032 | nM | 10.49 |
| CHEMBL4864274 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4877932 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4850513 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL4847056 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL4874151 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4868016 | — | IC50 | = | 2.25 | nM | 8.65 |
| CHEMBL4858923 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4853790 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4871481 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4845783 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4877484 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4847407 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4867946 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4860157 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4861377 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4869752 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4858509 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4866666 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4878889 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL4859853 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4860408 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL4846795 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4856214 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL4847413 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4862597 | — | IC50 | > | 20000.0 | nM | - |