Assay Detail
Binding
CHEMBL5515535
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Inhibition of TGFbetaR1 (unknown origin)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.55 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4778963 | — | — | 1 | 8.40 |
| CHEMBL185238 | GW786460X | — | 1 | 8.40 |
| CHEMBL1170377 | — | — | 1 | 7.92 |
| CHEMBL401570 | — | — | 1 | 7.84 |
| CHEMBL129677 | — | — | 1 | 7.60 |
| CHEMBL5095192 | PF-06952229 | 1.0 | 1 | 7.60 |
| CHEMBL4527908 | — | — | 1 | 7.52 |
| CHEMBL492634 | — | — | 1 | 7.44 |
| CHEMBL4594432 | LY-3200882 | 1.0 | 1 | 7.42 |
| CHEMBL260015 | — | — | 1 | 7.42 |
| CHEMBL4576703 | — | — | 1 | 7.41 |
| CHEMBL5518004 | — | — | 1 | 7.40 |
| CHEMBL1824446 | — | — | 1 | 7.33 |
| CHEMBL5559981 | — | — | 1 | 7.33 |
| CHEMBL238125 | — | — | 1 | 7.32 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 7.25 |
| CHEMBL261454 | — | — | 1 | 7.23 |
| CHEMBL440084 | SB-431542 | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4778963 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL185238 | GW786460X | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1170377 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL401570 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL129677 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5095192 | PF-06952229 | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4527908 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL492634 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4594432 | LY-3200882 | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL260015 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4576703 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5518004 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1824446 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5559981 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL238125 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL261454 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL440084 | SB-431542 | IC50 | = | 75.0 | nM | 7.12 |