Assay Detail
Binding
CHEMBL4739795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to RIOK3 (unknown origin)
34
Total Activities
17
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
Serine/threonine-protein kinase RIO3 (CHEMBL5659) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Compositions and methods for treating beta-globinopathies
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 34 | 6.41 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | 3.0 | 2 | 8.11 |
| CHEMBL1908397 | KW-2449 | 1.0 | 2 | 7.21 |
| CHEMBL388978 | STAUROSPORINE | — | 2 | 7.12 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 2 | 7.04 |
| CHEMBL475251 | R-406 | 2.0 | 2 | 6.70 |
| CHEMBL450786 | PHA-665752 | — | 2 | 6.41 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 2 | 6.40 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 2 | 6.22 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 2 | 6.20 |
| CHEMBL522892 | DOVITINIB | 3.0 | 2 | 6.20 |
| CHEMBL379218 | — | — | 2 | 6.20 |
| CHEMBL1289926 | AXITINIB | 4.0 | 2 | 6.00 |
| CHEMBL4762015 | — | — | 2 | 5.80 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 2 | 5.70 |
| CHEMBL1908842 | — | — | 2 | 5.70 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 2 | 5.64 |
| CHEMBL249697 | BMS-345541 | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.7 | nM | 8.11 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL1908397 | KW-2449 | Kd | = | 61.0 | nM | 7.21 |
| CHEMBL1908397 | KW-2449 | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL475251 | R-406 | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL475251 | R-406 | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL450786 | PHA-665752 | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL450786 | PHA-665752 | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 600.0 | nM | 6.22 |
| CHEMBL522892 | DOVITINIB | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL379218 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 650.0 | nM | 6.19 |
| CHEMBL379218 | — | Kd | = | 690.0 | nM | 6.16 |
| CHEMBL522892 | DOVITINIB | Kd | = | 690.0 | nM | 6.16 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL4762015 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL4762015 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1908842 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL1908842 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL249697 | BMS-345541 | Kd | > | 3162.28 | nM | - |
| CHEMBL249697 | BMS-345541 | Kd | > | 3000.0 | nM | - |