Assay Detail
Binding
CHEMBL4263978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ALK3 (unknown origin) using Ulight topo IIa (Thr 1342) peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr by TR-FRET analysis
24
Total Activities
24
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 |
Target
Bone morphogenetic protein receptor type-1A (CHEMBL5275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.68 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4280599 | — | — | 1 | 8.15 |
| CHEMBL513147 | — | — | 1 | 7.72 |
| CHEMBL4283587 | — | — | 1 | 6.35 |
| CHEMBL4281706 | — | — | 1 | 5.60 |
| CHEMBL4288921 | — | — | 1 | 5.46 |
| CHEMBL4283638 | — | — | 1 | 5.19 |
| CHEMBL4278763 | — | — | 1 | 5.09 |
| CHEMBL4291950 | — | — | 1 | 5.05 |
| CHEMBL4293917 | — | — | 1 | 4.89 |
| CHEMBL4285138 | — | — | 1 | 4.78 |
| CHEMBL4291891 | — | — | 1 | 4.19 |
| CHEMBL4288494 | — | — | 1 | - |
| CHEMBL4277180 | — | — | 1 | - |
| CHEMBL4292331 | — | — | 1 | - |
| CHEMBL4278242 | — | — | 1 | - |
| CHEMBL4280585 | — | — | 1 | - |
| CHEMBL4290804 | — | — | 1 | - |
| CHEMBL4277239 | — | — | 1 | - |
| CHEMBL4285523 | — | — | 1 | - |
| CHEMBL4278219 | — | — | 1 | - |
| CHEMBL4288905 | — | — | 1 | - |
| CHEMBL4283315 | — | — | 1 | - |
| CHEMBL4281166 | — | — | 1 | - |
| CHEMBL4279135 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4280599 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL513147 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4283587 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL4281706 | — | IC50 | = | 2534.0 | nM | 5.60 |
| CHEMBL4288921 | — | IC50 | = | 3466.0 | nM | 5.46 |
| CHEMBL4283638 | — | IC50 | = | 6439.0 | nM | 5.19 |
| CHEMBL4278763 | — | IC50 | = | 8195.0 | nM | 5.09 |
| CHEMBL4291950 | — | IC50 | = | 8897.0 | nM | 5.05 |
| CHEMBL4293917 | — | IC50 | = | 12830.0 | nM | 4.89 |
| CHEMBL4285138 | — | IC50 | = | 16550.0 | nM | 4.78 |
| CHEMBL4291891 | — | IC50 | = | 64750.0 | nM | 4.19 |
| CHEMBL4288494 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4277180 | — | IC50 | - | — | - | |
| CHEMBL4292331 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4278242 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4280585 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4290804 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4277239 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4285523 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4278219 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4288905 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4283315 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4281166 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4279135 | — | IC50 | > | 10000.0 | nM | - |