Assay Detail
Functional
CHEMBL4836067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human S1P2 receptor expressed in human CHO cells assessed as EC80 S1P-induced activation incubated for 4 hrs in presence of [35S]GTPgammaS by Topcount reader
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 36 | 7.99 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4864274 | — | — | 1 | 9.52 |
| CHEMBL4874736 | — | — | 1 | 9.49 |
| CHEMBL4877932 | — | — | 1 | 9.37 |
| CHEMBL4850513 | — | — | 1 | 9.21 |
| CHEMBL4847056 | — | — | 1 | 9.11 |
| CHEMBL4852127 | — | — | 1 | 9.10 |
| CHEMBL4874151 | — | — | 1 | 8.89 |
| CHEMBL4860509 | — | — | 1 | 8.68 |
| CHEMBL4868016 | — | — | 1 | 8.65 |
| CHEMBL4877928 | — | — | 1 | 8.51 |
| CHEMBL4867313 | — | — | 1 | 8.47 |
| CHEMBL4871414 | — | — | 1 | 8.28 |
| CHEMBL4873481 | — | — | 1 | 8.21 |
| CHEMBL4845863 | — | — | 1 | 8.15 |
| CHEMBL4864744 | — | — | 1 | 8.03 |
| 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 |
| CHEMBL4870007 | — | — | 1 | 7.51 |
| CHEMBL4860157 | — | — | 1 | 7.46 |
| CHEMBL4861377 | — | — | 1 | 7.44 |
| CHEMBL4869752 | — | — | 1 | 7.26 |
| CHEMBL4858509 | — | — | 1 | 6.98 |
| CHEMBL4866666 | — | — | 1 | 6.77 |
| CHEMBL4878889 | — | — | 1 | 6.62 |
| CHEMBL4859853 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4864274 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4874736 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4877932 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4850513 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL4847056 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL4852127 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4874151 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4860509 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4868016 | — | IC50 | = | 2.25 | nM | 8.65 |
| CHEMBL4877928 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4867313 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4871414 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4873481 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4845863 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4864744 | — | IC50 | = | 9.3 | nM | 8.03 |
| 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 |
| CHEMBL4870007 | — | IC50 | = | 31.0 | nM | 7.51 |
| 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 | = | 169.0 | nM | 6.77 |
| CHEMBL4878889 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL4859853 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4860408 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL4862597 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4847413 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4856214 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL4846795 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4876986 | — | IC50 | - | — | - |