Assay Detail
Functional
CHEMBL4701949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against HPASMC assessed as reduction in TGFbeta-induced cell proliferation measured after 48 hrs by CCK8 assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Pulmonary Artery Smooth Muscle Cells |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of Novel Pyrazolo[3,4-b] Pyridine Derivatives with Dual Activities of Vascular Remodeling Inhibition and Vasodilation for the Treatment of Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.45 | 4.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4785559 | — | — | 1 | 4.77 |
| CHEMBL4780823 | — | — | 1 | 4.69 |
| CHEMBL4749361 | — | — | 1 | 4.66 |
| CHEMBL4797223 | — | — | 1 | 4.65 |
| CHEMBL4761659 | — | — | 1 | 4.63 |
| CHEMBL4782536 | — | — | 1 | 4.61 |
| CHEMBL4754851 | — | — | 1 | 4.61 |
| CHEMBL4763850 | — | — | 1 | 4.60 |
| CHEMBL4761150 | — | — | 1 | 4.59 |
| CHEMBL4784189 | — | — | 1 | 4.53 |
| CHEMBL4752923 | — | — | 1 | 4.50 |
| CHEMBL4795950 | — | — | 1 | 4.46 |
| CHEMBL4764302 | — | — | 1 | 4.39 |
| CHEMBL4792492 | — | — | 1 | 4.28 |
| CHEMBL4782618 | — | — | 1 | 4.25 |
| CHEMBL4783763 | — | — | 1 | 4.23 |
| CHEMBL4743189 | — | — | 1 | 4.17 |
| CHEMBL4752719 | — | — | 1 | 4.17 |
| CHEMBL478629 | DORSOMORPHIN | — | 1 | 4.08 |
| CHEMBL4745236 | — | — | 1 | 4.05 |
| CHEMBL2107834 | RIOCIGUAT | 4.0 | 1 | - |
| CHEMBL4795558 | — | — | 1 | - |
| CHEMBL4749124 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4785559 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4780823 | — | IC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL4749361 | — | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL4797223 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL4761659 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL4782536 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL4754851 | — | IC50 | = | 24800.0 | nM | 4.61 |
| CHEMBL4763850 | — | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL4761150 | — | IC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL4784189 | — | IC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL4752923 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4795950 | — | IC50 | = | 34900.0 | nM | 4.46 |
| CHEMBL4764302 | — | IC50 | = | 40600.0 | nM | 4.39 |
| CHEMBL4792492 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL4782618 | — | IC50 | = | 56500.0 | nM | 4.25 |
| CHEMBL4783763 | — | IC50 | = | 59300.0 | nM | 4.23 |
| CHEMBL4743189 | — | IC50 | = | 68400.0 | nM | 4.17 |
| CHEMBL4752719 | — | IC50 | = | 67400.0 | nM | 4.17 |
| CHEMBL478629 | DORSOMORPHIN | IC50 | = | 82200.0 | nM | 4.08 |
| CHEMBL4745236 | — | IC50 | = | 89400.0 | nM | 4.05 |
| CHEMBL2107834 | RIOCIGUAT | IC50 | > | 100000.0 | nM | - |
| CHEMBL4795558 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4749124 | — | IC50 | > | 100000.0 | nM | - |