Assay Detail
Functional
CHEMBL4675902
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-stimulated [35S]GTPgammaS binding after 90 mins by scintillation counting method
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.88 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3718309 | — | — | 1 | 9.22 |
| CHEMBL4794652 | — | — | 1 | 8.30 |
| CHEMBL4776061 | — | — | 1 | 8.10 |
| CHEMBL3716446 | — | — | 1 | 8.10 |
| CHEMBL4750532 | — | — | 1 | 7.68 |
| CHEMBL3717201 | — | — | 1 | 7.66 |
| CHEMBL4755764 | — | — | 1 | 7.66 |
| CHEMBL3717853 | — | — | 1 | 7.60 |
| CHEMBL3717416 | — | — | 1 | 7.58 |
| CHEMBL3714917 | — | — | 1 | 7.30 |
| CHEMBL3716365 | GLPG-1205 | 2.0 | 1 | 7.27 |
| CHEMBL3719092 | — | — | 1 | 7.26 |
| CHEMBL4756307 | — | — | 1 | 7.20 |
| CHEMBL3718005 | — | — | 1 | 7.08 |
| CHEMBL3717363 | — | — | 1 | 6.99 |
| CHEMBL4744625 | — | — | 1 | 6.97 |
| CHEMBL4757870 | — | — | 1 | 6.81 |
| CHEMBL4795786 | — | — | 1 | 6.80 |
| CHEMBL3718710 | — | — | 1 | 6.67 |
| CHEMBL4799579 | — | — | 1 | 6.60 |
| CHEMBL3717307 | — | — | 1 | 6.56 |
| CHEMBL4760776 | — | — | 1 | 6.46 |
| CHEMBL4758226 | — | — | 1 | 6.42 |
| CHEMBL3718436 | — | — | 1 | 6.37 |
| CHEMBL3715879 | — | — | 1 | 6.33 |
| CHEMBL3716185 | — | — | 1 | 6.22 |
| CHEMBL4757413 | — | — | 1 | 6.22 |
| CHEMBL1871173 | — | — | 1 | 6.13 |
| CHEMBL4752941 | — | — | 1 | 6.09 |
| CHEMBL4748375 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3718309 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4794652 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3716446 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4776061 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4750532 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3717201 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4755764 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3717853 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3717416 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3714917 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3716365 | GLPG-1205 | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3719092 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4756307 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3718005 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3717363 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4744625 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4757870 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4795786 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL3718710 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL4799579 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL3717307 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4760776 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4758226 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL3718436 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL3715879 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL3716185 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL4757413 | — | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL1871173 | — | IC50 | = | 735.0 | nM | 6.13 |
| CHEMBL4752941 | — | IC50 | = | 808.0 | nM | 6.09 |
| CHEMBL4748375 | — | IC50 | = | 873.0 | nM | 6.06 |
| CHEMBL4794623 | — | IC50 | = | 1143.0 | nM | 5.94 |
| CHEMBL4795874 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL3717000 | — | IC50 | = | 3073.0 | nM | 5.51 |
| CHEMBL4783553 | — | IC50 | = | 8470.0 | nM | 5.07 |
| CHEMBL4743202 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4749530 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4742097 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4297635 | SETOGEPRAM | IC50 | > | 10000.0 | nM | - |