Assay Detail
Binding
CHEMBL3599868
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.29 | 5.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21333 | PRANLUKAST | 4.0 | 1 | 5.44 |
| CHEMBL603 | ZAFIRLUKAST | 4.0 | 1 | 5.13 |
| CHEMBL787 | MONTELUKAST | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21333 | PRANLUKAST | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL603 | ZAFIRLUKAST | IC50 | = | 7397.0 | nM | 5.13 |
| CHEMBL787 | MONTELUKAST | IC50 | > | 10000.0 | nM | - |