Assay Detail
Functional
CHEMBL1107780
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity at TGFBR1
45
Total Activities
24
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.02 | 8.00 |
| logIC50 | 18 | - | - |
| logKi | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229599 | — | — | 2 | 8.00 |
| CHEMBL387748 | — | — | 2 | 7.92 |
| CHEMBL376119 | — | — | 2 | 7.82 |
| CHEMBL389078 | — | — | 2 | 7.68 |
| CHEMBL226734 | — | — | 2 | 7.62 |
| CHEMBL229546 | — | — | 2 | 7.38 |
| CHEMBL387747 | — | — | 2 | 7.34 |
| CHEMBL229598 | — | — | 2 | 7.34 |
| CHEMBL229548 | — | — | 2 | 7.33 |
| CHEMBL229496 | — | — | 2 | 7.14 |
| CHEMBL229654 | — | — | 2 | 7.12 |
| CHEMBL226733 | — | — | 1 | 7.04 |
| CHEMBL440084 | SB-431542 | — | 2 | 7.03 |
| CHEMBL229547 | — | — | 2 | 6.92 |
| CHEMBL445934 | — | — | 2 | 6.82 |
| CHEMBL6250 | — | — | 2 | 6.77 |
| CHEMBL229495 | — | — | 2 | 6.77 |
| CHEMBL229597 | — | — | 2 | 6.58 |
| CHEMBL267228 | — | — | 2 | 6.58 |
| CHEMBL229497 | — | — | 2 | 6.44 |
| CHEMBL389079 | — | — | 2 | 6.42 |
| CHEMBL269339 | — | — | 1 | 5.82 |
| CHEMBL269341 | — | — | 2 | 5.53 |
| CHEMBL226838 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229599 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL387748 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL376119 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL389078 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL226734 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL229546 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL387747 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL229598 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL229548 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL229496 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL229654 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL226733 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL440084 | SB-431542 | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL229547 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL445934 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL6250 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL229495 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL267228 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL229597 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL229497 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL389079 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL269339 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL269341 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL387748 | — | logIC50 | = | -1.921 | — | - |
| CHEMBL267228 | — | logKi | = | -0.585 | — | - |
| CHEMBL440084 | SB-431542 | logKi | = | -1.027 | — | - |
| CHEMBL229548 | — | logKi | = | -1.32 | — | - |
| CHEMBL229599 | — | logKi | = | -2.0 | — | - |
| CHEMBL6250 | — | logIC50 | = | -0.77 | — | - |
| CHEMBL269341 | — | logIC50 | = | 0.4698 | — | - |
| CHEMBL387747 | — | logIC50 | = | -1.337 | — | - |
| CHEMBL229495 | — | logIC50 | = | -0.759 | — | - |
| CHEMBL229496 | — | logIC50 | = | -1.137 | — | - |
| CHEMBL229497 | — | logIC50 | = | -0.4434 | — | - |
| CHEMBL445934 | — | logIC50 | = | -0.815 | — | - |
| CHEMBL229546 | — | logIC50 | = | -1.377 | — | - |
| CHEMBL229547 | — | logIC50 | = | -0.924 | — | - |
| CHEMBL389078 | — | logIC50 | = | -1.678 | — | - |
| CHEMBL229597 | — | logIC50 | = | -0.582 | — | - |
| CHEMBL229598 | — | logIC50 | = | -1.337 | — | - |
| CHEMBL389079 | — | logIC50 | = | -0.415 | — | - |
| CHEMBL229654 | — | logIC50 | = | -1.125 | — | - |
| CHEMBL376119 | — | logIC50 | = | -1.824 | — | - |
| CHEMBL226734 | — | logIC50 | = | -1.62 | — | - |
| CHEMBL226838 | — | logIC50 | = | -1.328 | — | - |