Assay Detail
Binding
CHEMBL5319643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant C-terminal 6His-tagged human BMPR2 (188 to 517 residues) expressed in Escherichia coli Rosetta assessed as apparent inhibition constant using ATP as substrate incubated for 30 mins by Morrison plot analysis
26
Total Activities
26
Compounds Tested
2
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-2 (CHEMBL5467) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.26 | 8.30 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5404016 | — | — | 1 | 8.30 |
| CHEMBL5404269 | — | — | 1 | 8.21 |
| CHEMBL5422418 | — | — | 1 | 8.15 |
| CHEMBL5434353 | — | — | 1 | 8.10 |
| CHEMBL5420022 | — | — | 1 | 7.80 |
| CHEMBL5437902 | — | — | 1 | 7.75 |
| CHEMBL5398151 | — | — | 1 | 7.69 |
| CHEMBL5436042 | — | — | 1 | 7.66 |
| CHEMBL5428614 | — | — | 1 | 7.41 |
| CHEMBL5402879 | — | — | 1 | 7.40 |
| CHEMBL5421520 | — | — | 1 | 7.06 |
| CHEMBL5409160 | — | — | 1 | 6.93 |
| CHEMBL5408480 | — | — | 1 | 6.66 |
| CHEMBL5397482 | — | — | 1 | 6.66 |
| CHEMBL5399442 | — | — | 1 | 6.63 |
| CHEMBL5400260 | — | — | 1 | 6.60 |
| CHEMBL5438139 | — | — | 1 | 6.51 |
| CHEMBL5411422 | — | — | 1 | 6.37 |
| CHEMBL5434246 | — | — | 1 | 6.03 |
| CHEMBL5420069 | — | — | 1 | - |
| CHEMBL5435399 | — | — | 1 | - |
| CHEMBL5433406 | — | — | 1 | - |
| CHEMBL5411287 | — | — | 1 | - |
| CHEMBL5420892 | — | — | 1 | - |
| CHEMBL5438355 | — | — | 1 | - |
| CHEMBL5417301 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5404016 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5404269 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL5422418 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5434353 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5420022 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5437902 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5398151 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL5436042 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5428614 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL5402879 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL5421520 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL5409160 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL5408480 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5397482 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5399442 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL5400260 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL5438139 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL5411422 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL5434246 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL5420069 | — | Inhibition | - | % | - | |
| CHEMBL5435399 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5433406 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5411287 | — | Inhibition | - | % | - | |
| CHEMBL5420892 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5438355 | — | Ki | > | 200.0 | nM | - |
| CHEMBL5417301 | — | Ki | > | 200.0 | nM | - |