Assay Detail
Binding
CHEMBL4402235
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length human His6-tagged HPGDS expressed in Escherichia coli BL21 (DE3) using PGH2 as substrate measured after 90 to 120 secs by RapidFire high-throughput mass spectrometry assay
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Hematopoietic prostaglandin D synthase (CHEMBL5879) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 74 | 6.48 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439454 | — | — | 1 | 8.09 |
| CHEMBL4452633 | — | — | 1 | 8.01 |
| CHEMBL4473072 | — | — | 1 | 8.00 |
| CHEMBL4454901 | — | — | 1 | 7.85 |
| CHEMBL4526974 | — | — | 1 | 7.82 |
| CHEMBL4530713 | — | — | 1 | 7.80 |
| CHEMBL4443093 | — | — | 1 | 7.77 |
| CHEMBL4458862 | — | — | 1 | 7.70 |
| CHEMBL4467696 | — | — | 1 | 7.64 |
| CHEMBL4483631 | — | — | 1 | 7.60 |
| CHEMBL4463046 | — | — | 1 | 7.58 |
| CHEMBL4454083 | — | — | 1 | 7.31 |
| CHEMBL4441669 | — | — | 1 | 7.28 |
| CHEMBL4483661 | — | — | 1 | 7.25 |
| CHEMBL4564218 | — | — | 1 | 7.24 |
| CHEMBL4435792 | — | — | 1 | 7.24 |
| CHEMBL4544169 | — | — | 1 | 7.15 |
| CHEMBL4476572 | — | — | 1 | 7.14 |
| CHEMBL4573375 | — | — | 1 | 7.11 |
| CHEMBL4461589 | — | — | 1 | 7.01 |
| CHEMBL4438813 | — | — | 1 | 7.00 |
| CHEMBL4446601 | — | — | 1 | 6.96 |
| CHEMBL4591235 | — | — | 1 | 6.96 |
| CHEMBL4476594 | — | — | 1 | 6.92 |
| CHEMBL4584855 | — | — | 1 | 6.92 |
| CHEMBL4539130 | — | — | 1 | 6.80 |
| CHEMBL4567043 | — | — | 1 | 6.77 |
| CHEMBL4580109 | — | — | 1 | 6.70 |
| CHEMBL4571908 | — | — | 1 | 6.70 |
| CHEMBL4555427 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439454 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4452633 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4473072 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4454901 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4526974 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4530713 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4443093 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4458862 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4467696 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4483631 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4463046 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4454083 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4441669 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4483661 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4435792 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4564218 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4544169 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4476572 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4573375 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4461589 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4438813 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4446601 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4591235 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4476594 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4584855 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4539130 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4567043 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4580109 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4571908 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4555427 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4461716 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4469614 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4570414 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4520564 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4446712 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4469436 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4520607 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4521862 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4547202 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4547648 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4550149 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4525227 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4563481 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4468172 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4552112 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4575981 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4547156 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4588916 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4461342 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4476387 | — | IC50 | = | 870.0 | nM | 6.06 |