Assay Detail
Functional
CHEMBL1781819
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Antagonist activity at human CRTH2 receptor expressed in HEK293-EBNA cells assessed as inhibition of forskolin-stimulated intracellular cAMP production by [125I]-cAMP scintillation proximity assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293-EBNA |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New indole amide derivatives as potent CRTH2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.29 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1778523 | — | — | 1 | 8.70 |
| CHEMBL1778387 | — | — | 1 | 8.52 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.52 |
| CHEMBL1778388 | — | — | 1 | 8.40 |
| CHEMBL1778524 | — | — | 1 | 8.40 |
| CHEMBL1778522 | — | — | 1 | 8.21 |
| CHEMBL1778525 | — | — | 1 | 8.10 |
| CHEMBL1778506 | — | — | 1 | 7.92 |
| CHEMBL1778505 | — | — | 1 | 7.60 |
| CHEMBL1778521 | — | — | 1 | 7.52 |
| CHEMBL1778508 | — | — | 1 | 6.85 |
| CHEMBL1778390 | — | — | 1 | 6.27 |
| CHEMBL1778510 | — | — | 1 | 6.20 |
| CHEMBL1778507 | — | — | 1 | 6.09 |
| CHEMBL1778504 | — | — | 1 | 5.68 |
| CHEMBL1778389 | — | — | 1 | 5.60 |
| CHEMBL1778509 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1778523 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1778387 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL561132 | MK-7246 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1778388 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1778524 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1778522 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1778525 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1778506 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1778505 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1778521 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1778508 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1778390 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1778510 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1778507 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL1778504 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1778389 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1778509 | — | IC50 | = | 3700.0 | nM | 5.43 |