Assay Detail
Functional
CHEMBL3404758
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Antagonist activity at human CysLT1 receptor expressed in CHO 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 | CHO |
| 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 | 7.36 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3403186 | — | — | 1 | 9.23 |
| CHEMBL3401689 | — | — | 1 | 9.10 |
| CHEMBL3342955 | — | — | 1 | 7.96 |
| CHEMBL3403190 | — | — | 1 | 7.89 |
| CHEMBL3401690 | — | — | 1 | 7.66 |
| CHEMBL3403187 | — | — | 1 | 7.62 |
| CHEMBL3403185 | — | — | 1 | 7.46 |
| CHEMBL3401686 | — | — | 1 | 7.24 |
| CHEMBL3401687 | — | — | 1 | 7.16 |
| CHEMBL3401691 | — | — | 1 | 7.16 |
| CHEMBL3401688 | — | — | 1 | 7.09 |
| CHEMBL3403188 | — | — | 1 | 6.60 |
| CHEMBL3403189 | — | — | 1 | 6.31 |
| CHEMBL3403184 | — | — | 1 | 6.13 |
| CHEMBL3401692 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3403186 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL3401689 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3342955 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3403190 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3401690 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3403187 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3403185 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3401686 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3401687 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3401691 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3401688 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3403188 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3403189 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3403184 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3401692 | — | IC50 | = | 1900.0 | nM | 5.72 |