Assay Detail
Binding
CHEMBL1908656
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Binding constant for MAP4K2 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
Mitogen-activated protein kinase kinase kinase kinase 2 (CHEMBL5330) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.36 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.51 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.33 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.06 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.96 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.48 |
| CHEMBL1908395 | — | — | 1 | 7.19 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.10 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 7.05 |
| CHEMBL1241674 | — | — | 1 | 7.00 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.00 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.72 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.66 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.54 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.54 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.48 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.27 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.17 |
| CHEMBL386051 | — | — | 1 | 5.92 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.89 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.89 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 5.80 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.77 |
| CHEMBL379218 | — | — | 1 | 5.72 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.72 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 5.70 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 5.70 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.68 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.60 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 5.58 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288441 | BOSUTINIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 4.7 | nM | 8.33 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 8.8 | nM | 8.06 |
| CHEMBL1908397 | KW-2449 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL535 | SUNITINIB | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL1908395 | — | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 89.0 | nM | 7.05 |
| CHEMBL1241674 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL574738 | AST-487 | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL509032 | TAE-684 | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL180022 | NERATINIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL31965 | CANERTINIB | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 540.0 | nM | 6.27 |
| CHEMBL475251 | R-406 | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL386051 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL1721885 | SU-014813 | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL379218 | — | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1230609 | FORETINIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2100.0 | nM | 5.68 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL384304 | RG-547 | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL450786 | PHA-665752 | Kd | = | 3600.0 | nM | 5.44 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 4800.0 | nM | 5.32 |
| CHEMBL558752 | RAF-265 | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908396 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1230020 | PLX-4720 | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |