Assay Detail
Binding
CHEMBL5265274
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of H-PGDS in rat RBL cells assessed as reduction in A23187-induced PGD2 production pretreated for 30 mins followed by A23187 addition for 30 mins by RapidFire Mass spectrometry
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | RBL |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Hematopoietic prostaglandin D synthase (CHEMBL4523131) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 63 | 6.70 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5279371 | — | — | 1 | 8.43 |
| CHEMBL5267588 | — | — | 1 | 8.42 |
| CHEMBL5289730 | — | — | 1 | 8.41 |
| CHEMBL5272869 | — | — | 1 | 8.41 |
| CHEMBL5278680 | — | — | 1 | 8.33 |
| CHEMBL5269778 | — | — | 1 | 8.28 |
| CHEMBL5282861 | — | — | 1 | 7.96 |
| CHEMBL5266142 | — | — | 1 | 7.85 |
| CHEMBL5285125 | — | — | 1 | 7.85 |
| CHEMBL5277213 | — | — | 1 | 7.66 |
| CHEMBL5279860 | — | — | 1 | 7.62 |
| CHEMBL5290809 | — | — | 1 | 7.55 |
| CHEMBL5279720 | — | — | 1 | 7.54 |
| CHEMBL5275536 | — | — | 1 | 7.50 |
| CHEMBL5285108 | — | — | 1 | 7.38 |
| CHEMBL5269001 | — | — | 1 | 7.30 |
| CHEMBL5266974 | — | — | 1 | 7.30 |
| CHEMBL5268479 | — | — | 1 | 7.27 |
| CHEMBL5289474 | — | — | 1 | 7.19 |
| CHEMBL5283521 | — | — | 1 | 7.12 |
| CHEMBL5288898 | — | — | 1 | 7.06 |
| CHEMBL5271855 | — | — | 1 | 7.03 |
| CHEMBL4483631 | — | — | 1 | 7.00 |
| CHEMBL5284902 | — | — | 1 | 6.96 |
| CHEMBL5288532 | — | — | 1 | 6.92 |
| CHEMBL5274762 | — | — | 1 | 6.82 |
| CHEMBL4473072 | — | — | 1 | 6.80 |
| CHEMBL5278530 | — | — | 1 | 6.77 |
| CHEMBL5282228 | — | — | 1 | 6.77 |
| CHEMBL5276706 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5279371 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5267588 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5272869 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5289730 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5278680 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5269778 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5282861 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5266142 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5285125 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5277213 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5279860 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5290809 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5279720 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5275536 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5285108 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5269001 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5266974 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5268479 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5289474 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5283521 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5288898 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5271855 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4483631 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5284902 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5288532 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5274762 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4473072 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5278530 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5282228 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5276706 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5273656 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5282346 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5280247 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5270752 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5274007 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5290969 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5283878 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5289296 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5272443 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5275367 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5274174 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5284347 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5282999 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5290010 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5284243 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5283710 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5280283 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5283830 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5273807 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5267306 | — | EC50 | = | 3000.0 | nM | 5.52 |