Assay Detail
Functional
CHEMBL861567
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TGFbeta R1 induced transcriptional activation of p3TP-Lux in mink Mv1Lu lung cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mustela |
| Cell Type | Mv1Lu |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.88 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204170 | — | — | 1 | 8.10 |
| CHEMBL382838 | — | — | 1 | 7.82 |
| CHEMBL204966 | — | — | 1 | 7.54 |
| CHEMBL261454 | — | — | 1 | 7.40 |
| CHEMBL377711 | — | — | 1 | 7.29 |
| CHEMBL441176 | — | — | 1 | 7.28 |
| CHEMBL204063 | — | — | 1 | 7.11 |
| CHEMBL203619 | — | — | 1 | 7.10 |
| CHEMBL203791 | — | — | 1 | 7.00 |
| CHEMBL202730 | — | — | 1 | 6.98 |
| CHEMBL206233 | — | — | 1 | 6.93 |
| CHEMBL381532 | — | — | 1 | 6.73 |
| CHEMBL378167 | — | — | 1 | 6.65 |
| CHEMBL204139 | — | — | 1 | 6.38 |
| CHEMBL203214 | — | — | 1 | 5.86 |
| CHEMBL202625 | — | — | 1 | 5.61 |
| CHEMBL204158 | — | — | 1 | 5.23 |
| CHEMBL427211 | — | — | 1 | - |
| CHEMBL377717 | — | — | 1 | - |
| CHEMBL204061 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204170 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL382838 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL204966 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL261454 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL377711 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL441176 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL204063 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL203619 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL203791 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL202730 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL206233 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL381532 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL378167 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL204139 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL203214 | — | IC50 | = | 1373.0 | nM | 5.86 |
| CHEMBL202625 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL204158 | — | IC50 | = | 5890.0 | nM | 5.23 |
| CHEMBL427211 | — | IC50 | - | — | - | |
| CHEMBL377717 | — | IC50 | - | — | - | |
| CHEMBL204061 | — | IC50 | - | — | - |