Assay Detail
Binding
CHEMBL1908709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for GAK 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 |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.80 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 8.96 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.89 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.59 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.51 |
| CHEMBL509032 | TAE-684 | — | 1 | 8.28 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.14 |
| CHEMBL386051 | — | — | 1 | 8.09 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.89 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.77 |
| CHEMBL10 | SB-203580 | — | 1 | 7.72 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.70 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 7.36 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.10 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.07 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.00 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.00 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 6.75 |
| CHEMBL379218 | — | — | 1 | 6.75 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.70 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.60 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.60 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.58 |
| CHEMBL464552 | — | — | 1 | 6.57 |
| CHEMBL1241674 | — | — | 1 | 6.50 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 6.43 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.42 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.31 |
| CHEMBL1908395 | — | — | 1 | 6.06 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.00 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL553 | ERLOTINIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL509032 | TAE-684 | Kd | = | 5.3 | nM | 8.28 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.3 | nM | 8.14 |
| CHEMBL386051 | — | Kd | = | 8.2 | nM | 8.09 |
| CHEMBL939 | GEFITINIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL10 | SB-203580 | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL535 | SUNITINIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL1721885 | SU-014813 | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL1173655 | AFATINIB | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL24828 | VANDETANIB | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 99.0 | nM | 7.00 |
| CHEMBL31965 | CANERTINIB | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL513909 | BI-2536 | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL379218 | — | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL475251 | R-406 | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL180022 | NERATINIB | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL1908397 | KW-2449 | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL464552 | — | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL1241674 | — | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL522892 | DOVITINIB | Kd | = | 490.0 | nM | 6.31 |
| CHEMBL1908395 | — | Kd | = | 870.0 | nM | 6.06 |
| CHEMBL941 | IMATINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL574738 | AST-487 | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL450786 | PHA-665752 | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL230011 | TG100-115 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL1908396 | — | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL296468 | BMS-387032 | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL223360 | LINIFANIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL521851 | PICTILISIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL1289926 | AXITINIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 3700.0 | nM | 5.43 |
| CHEMBL103667 | DORAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL1230020 | PLX-4720 | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |