Assay Detail
Binding
CHEMBL1908661
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Binding constant for DYRK1B kinase domain
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1B (CHEMBL5543) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.17 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379218 | — | — | 1 | 8.41 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.55 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.54 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 7.08 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 6.70 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 6.60 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 6.54 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.48 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 6.14 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.03 |
| CHEMBL464552 | — | — | 1 | 6.01 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 6.00 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.80 |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | 5.75 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.64 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.58 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.55 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 5.42 |
| CHEMBL509032 | TAE-684 | — | 1 | 5.35 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 5.27 |
| CHEMBL573339 | PI-103 | — | 1 | 5.24 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.02 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL608154 | — | — | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL105442 | CI-1040 | 2.0 | 1 | - |
| CHEMBL10 | SB-203580 | — | 1 | - |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379218 | — | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 84.0 | nM | 7.08 |
| CHEMBL296468 | BMS-387032 | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL384304 | RG-547 | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL445813 | AT-7519 | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL230011 | TG100-115 | Kd | = | 730.0 | nM | 6.14 |
| CHEMBL1908397 | KW-2449 | Kd | = | 940.0 | nM | 6.03 |
| CHEMBL464552 | — | Kd | = | 970.0 | nM | 6.01 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL1236107 | SGX-523 | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL535 | SUNITINIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL1721885 | SU-014813 | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL1173655 | AFATINIB | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL521851 | PICTILISIB | Kd | = | 3800.0 | nM | 5.42 |
| CHEMBL509032 | TAE-684 | Kd | = | 4500.0 | nM | 5.35 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 5400.0 | nM | 5.27 |
| CHEMBL573339 | PI-103 | Kd | = | 5700.0 | nM | 5.24 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL574738 | AST-487 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL386051 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL450786 | PHA-665752 | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |