Assay Detail
Binding
CHEMBL4378183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His6-tagged LTC4S expressed in Pichia pastoris X33 using LTA4 methyl ester and glutathione as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by LC-MS/MS analysis
34
Total Activities
34
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 |
Publication
Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1<i>S</i>,2<i>S</i>)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.39 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3903201 | — | — | 1 | 9.60 |
| CHEMBL3961833 | AZD-9898 | 1.0 | 1 | 9.55 |
| CHEMBL4549822 | — | — | 1 | 9.55 |
| CHEMBL4567083 | — | — | 1 | 9.44 |
| CHEMBL4464773 | — | — | 1 | 9.42 |
| CHEMBL4562583 | — | — | 1 | 9.22 |
| CHEMBL4563433 | — | — | 1 | 9.20 |
| CHEMBL4584584 | — | — | 1 | 9.20 |
| CHEMBL3971210 | — | — | 1 | 9.18 |
| CHEMBL4574439 | — | — | 1 | 9.15 |
| CHEMBL4441362 | — | — | 1 | 9.12 |
| CHEMBL4476024 | — | — | 1 | 8.98 |
| CHEMBL4454609 | — | — | 1 | 8.85 |
| CHEMBL4545014 | — | — | 1 | 8.71 |
| CHEMBL4545950 | — | — | 1 | 8.68 |
| CHEMBL4525972 | — | — | 1 | 8.62 |
| CHEMBL4467942 | — | — | 1 | 8.43 |
| CHEMBL4574370 | — | — | 1 | 8.32 |
| CHEMBL4442047 | — | — | 1 | 8.31 |
| CHEMBL4576647 | — | — | 1 | 8.28 |
| CHEMBL4567339 | — | — | 1 | 8.19 |
| CHEMBL4439499 | — | — | 1 | 8.10 |
| CHEMBL4439148 | — | — | 1 | 8.06 |
| CHEMBL4445815 | — | — | 1 | 7.94 |
| CHEMBL4531985 | — | — | 1 | 7.89 |
| CHEMBL4565208 | — | — | 1 | 7.87 |
| CHEMBL4456770 | — | — | 1 | 7.81 |
| CHEMBL4465323 | — | — | 1 | 7.61 |
| CHEMBL4440468 | — | — | 1 | 7.56 |
| CHEMBL4466708 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3903201 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3961833 | AZD-9898 | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4549822 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4567083 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4464773 | — | IC50 | = | 0.381 | nM | 9.42 |
| CHEMBL4562583 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4563433 | — | IC50 | = | 0.626 | nM | 9.20 |
| CHEMBL4584584 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL3971210 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4574439 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4441362 | — | IC50 | = | 0.758 | nM | 9.12 |
| CHEMBL4476024 | — | IC50 | = | 1.05 | nM | 8.98 |
| CHEMBL4454609 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4545014 | — | IC50 | = | 1.97 | nM | 8.71 |
| CHEMBL4545950 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL4525972 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4467942 | — | IC50 | = | 3.71 | nM | 8.43 |
| CHEMBL4574370 | — | IC50 | = | 4.74 | nM | 8.32 |
| CHEMBL4442047 | — | IC50 | = | 4.94 | nM | 8.31 |
| CHEMBL4576647 | — | IC50 | = | 5.26 | nM | 8.28 |
| CHEMBL4567339 | — | IC50 | = | 6.42 | nM | 8.19 |
| CHEMBL4439499 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4439148 | — | IC50 | = | 8.65 | nM | 8.06 |
| CHEMBL4445815 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4531985 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4565208 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL4456770 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL4465323 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL4440468 | — | IC50 | = | 27.4 | nM | 7.56 |
| CHEMBL4466708 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL4460916 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4565235 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4440339 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4457672 | — | IC50 | = | 1900.0 | nM | 5.72 |