Assay Detail
Binding
CHEMBL2390518
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Inhibition of TGFBR2 (unknown origin)
11
Total Activities
11
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
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.38 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2385579 | — | — | 1 | 8.86 |
| CHEMBL2385596 | — | — | 1 | 7.82 |
| CHEMBL2385600 | — | — | 1 | 7.80 |
| CHEMBL2385582 | — | — | 1 | 7.58 |
| CHEMBL2385586 | — | — | 1 | 7.42 |
| CHEMBL478629 | DORSOMORPHIN | — | 1 | 6.99 |
| CHEMBL513147 | — | — | 1 | 6.85 |
| CHEMBL511563 | — | — | 1 | 6.63 |
| CHEMBL2385591 | — | — | 1 | 6.49 |
| CHEMBL502351 | — | — | 1 | - |
| CHEMBL2385597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2385579 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL2385596 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2385600 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2385582 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2385586 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL478629 | DORSOMORPHIN | IC50 | = | 102.9 | nM | 6.99 |
| CHEMBL513147 | — | IC50 | = | 140.4 | nM | 6.85 |
| CHEMBL511563 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL2385591 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL502351 | — | IC50 | - | — | - | |
| CHEMBL2385597 | — | IC50 | - | — | - |