Assay Detail
Functional
CHEMBL1646947
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Antagonist activity at human CRTH2 expressed in HEK293 cells assessed as inhibition of forskolin-induced increase intracellular [125I]cAMP level by scintillation proximity assay
13
Total Activities
13
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
Azaindoles as potent CRTH2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.12 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.52 |
| CHEMBL1641809 | — | — | 1 | 8.49 |
| CHEMBL1641808 | — | — | 1 | 8.47 |
| CHEMBL1641813 | — | — | 1 | 8.46 |
| CHEMBL1641810 | — | — | 1 | 8.44 |
| CHEMBL1641815 | — | — | 1 | 8.36 |
| CHEMBL1641817 | — | — | 1 | 8.35 |
| CHEMBL1641816 | — | — | 1 | 8.33 |
| CHEMBL1641811 | — | — | 1 | 8.24 |
| CHEMBL1641818 | — | — | 1 | 8.15 |
| CHEMBL1641814 | — | — | 1 | 8.12 |
| CHEMBL1641812 | — | — | 1 | 7.13 |
| CHEMBL1641807 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL561132 | MK-7246 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1641809 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1641808 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1641813 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1641810 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1641815 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1641817 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1641816 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL1641811 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1641818 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1641814 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL1641812 | — | IC50 | = | 73.8 | nM | 7.13 |
| CHEMBL1641807 | — | IC50 | = | 351.0 | nM | 6.46 |