Assay Detail
Binding
CHEMBL1908418
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Binding constant for MEK5 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 mitogen-activated protein kinase kinase 5 (CHEMBL4948) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 7.00 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230020 | PLX-4720 | — | 1 | 9.80 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.74 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.60 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 8.55 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.54 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.48 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.15 |
| CHEMBL1241674 | — | — | 1 | 8.14 |
| CHEMBL1908396 | — | — | 1 | 8.13 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.09 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.50 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.39 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.34 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.31 |
| CHEMBL386051 | — | — | 1 | 7.24 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.22 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.20 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.13 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 7.12 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.02 |
| CHEMBL1908395 | — | — | 1 | 7.00 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.92 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.85 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 6.75 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.72 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.72 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.70 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.58 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.44 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230020 | PLX-4720 | Kd | = | 0.16 | nM | 9.80 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL1230609 | FORETINIB | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 2.8 | nM | 8.55 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 2.9 | nM | 8.54 |
| CHEMBL5416410 | DASATINIB | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL1241674 | — | Kd | = | 7.3 | nM | 8.14 |
| CHEMBL1908396 | — | Kd | = | 7.4 | nM | 8.13 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 8.2 | nM | 8.09 |
| CHEMBL522892 | DOVITINIB | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL475251 | R-406 | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL535 | SUNITINIB | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL24828 | VANDETANIB | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL386051 | — | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL31965 | CANERTINIB | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL180022 | NERATINIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL574738 | AST-487 | Kd | = | 74.0 | nM | 7.13 |
| CHEMBL1721885 | SU-014813 | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL553 | ERLOTINIB | Kd | = | 96.0 | nM | 7.02 |
| CHEMBL1908395 | — | Kd | = | 99.0 | nM | 7.00 |
| CHEMBL1908397 | KW-2449 | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL1289926 | AXITINIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL1336 | SORAFENIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL255863 | NILOTINIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL509032 | TAE-684 | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 480.0 | nM | 6.32 |
| CHEMBL939 | GEFITINIB | Kd | = | 600.0 | nM | 6.22 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL554 | LAPATINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL223360 | LINIFANIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL1173655 | AFATINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL10 | SB-203580 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL450786 | PHA-665752 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL558752 | RAF-265 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL377300 | BRIVANIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL525191 | — | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |