Assay Detail
Binding
CHEMBL1048115
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Inhibition of TGFR1
104
Total Activities
104
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-beta type I receptor (ALK5) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 104 | 6.80 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL185238 | GW786460X | — | 1 | 8.40 |
| CHEMBL576062 | — | — | 1 | 8.22 |
| CHEMBL229599 | — | — | 1 | 8.00 |
| CHEMBL361237 | GW785804X | — | 1 | 7.96 |
| CHEMBL365663 | GW780159X | — | 1 | 7.89 |
| CHEMBL567706 | — | — | 1 | 7.82 |
| CHEMBL565814 | — | — | 1 | 7.75 |
| CHEMBL202887 | — | — | 1 | 7.75 |
| CHEMBL183354 | — | — | 1 | 7.72 |
| CHEMBL181361 | GW693481X | — | 1 | 7.70 |
| CHEMBL229597 | — | — | 1 | 7.68 |
| CHEMBL445934 | — | — | 1 | 7.62 |
| CHEMBL383523 | — | — | 1 | 7.62 |
| CHEMBL202943 | — | — | 1 | 7.60 |
| CHEMBL585505 | — | — | 1 | 7.60 |
| CHEMBL568357 | — | — | 1 | 7.57 |
| CHEMBL565643 | — | — | 1 | 7.52 |
| CHEMBL208437 | GW711782X | — | 1 | 7.52 |
| CHEMBL118928 | — | — | 1 | 7.51 |
| CHEMBL585117 | — | — | 1 | 7.50 |
| CHEMBL565645 | — | — | 1 | 7.47 |
| CHEMBL437118 | — | — | 1 | 7.46 |
| CHEMBL584928 | — | — | 1 | 7.40 |
| CHEMBL202994 | — | — | 1 | 7.40 |
| CHEMBL204063 | — | — | 1 | 7.39 |
| CHEMBL203162 | — | — | 1 | 7.38 |
| CHEMBL204838 | — | — | 1 | 7.37 |
| CHEMBL229495 | — | — | 1 | 7.34 |
| CHEMBL389079 | — | — | 1 | 7.34 |
| CHEMBL330814 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL185238 | GW786460X | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL576062 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL229599 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL361237 | GW785804X | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL365663 | GW780159X | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL567706 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL565814 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL202887 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL183354 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL181361 | GW693481X | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL229597 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL445934 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL383523 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL585505 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL202943 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL568357 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL565643 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL208437 | GW711782X | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL118928 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL585117 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL565645 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL437118 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL584928 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL202994 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL204063 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL203162 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL204838 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL389079 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL229495 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL330814 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL229548 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL566234 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL381948 | GW680975X | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL332344 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL261454 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL121554 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL585700 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL205427 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL259821 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL381532 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL122583 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL229496 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL229654 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL119976 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL566439 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL379700 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL565815 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL120587 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL205151 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL340203 | — | IC50 | = | 91.0 | nM | 7.04 |