Assay Detail
Binding
CHEMBL1908409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for DYRK1A 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 1A (CHEMBL2292) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.65 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379218 | — | — | 1 | 8.68 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.40 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.70 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 7.64 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 7.11 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.00 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 6.92 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 6.80 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.75 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.70 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.60 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.58 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.58 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 6.47 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 6.17 |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | 6.11 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 6.04 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.01 |
| CHEMBL464552 | — | — | 1 | 5.92 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 5.82 |
| CHEMBL608154 | — | — | 1 | 5.68 |
| CHEMBL1241674 | — | — | 1 | 5.64 |
| CHEMBL509032 | TAE-684 | — | 1 | 5.54 |
| CHEMBL261849 | GW632580X | — | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379218 | — | Kd | = | 2.1 | nM | 8.68 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL384304 | RG-547 | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL445813 | AT-7519 | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL1908397 | KW-2449 | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL535 | SUNITINIB | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL475251 | R-406 | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL1721885 | SU-014813 | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL296468 | BMS-387032 | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL230011 | TG100-115 | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL1236107 | SGX-523 | Kd | = | 780.0 | nM | 6.11 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 910.0 | nM | 6.04 |
| CHEMBL1173655 | AFATINIB | Kd | = | 970.0 | nM | 6.01 |
| CHEMBL464552 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL31965 | CANERTINIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL608154 | — | Kd | = | 2100.0 | nM | 5.68 |
| CHEMBL1241674 | — | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL509032 | TAE-684 | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL574738 | AST-487 | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL386051 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |