Assay Detail
Functional
CHEMBL3404759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a potent, orally available dual CysLT₁ and CysLT₂ antagonist with dicarboxylic acid.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.75 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3403187 | — | — | 1 | 9.51 |
| CHEMBL3401689 | — | — | 1 | 9.31 |
| CHEMBL3342955 | — | — | 1 | 8.60 |
| CHEMBL3403186 | — | — | 1 | 8.47 |
| CHEMBL3401687 | — | — | 1 | 8.24 |
| CHEMBL3401691 | — | — | 1 | 8.24 |
| CHEMBL3403185 | — | — | 1 | 7.82 |
| CHEMBL3401688 | — | — | 1 | 7.80 |
| CHEMBL3401690 | — | — | 1 | 7.80 |
| CHEMBL3403190 | — | — | 1 | 7.60 |
| CHEMBL3401686 | — | — | 1 | 7.52 |
| CHEMBL3403189 | — | — | 1 | 7.12 |
| CHEMBL3403188 | — | — | 1 | 6.43 |
| CHEMBL3403184 | — | — | 1 | 6.39 |
| CHEMBL3401692 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3403187 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL3401689 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3342955 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3403186 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3401687 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3401691 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3403185 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3401688 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3401690 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3403190 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3401686 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3403189 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3403188 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3403184 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3401692 | — | IC50 | = | 4300.0 | nM | 5.37 |