Assay Detail
Binding
CHEMBL1908678
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for ABL1(F317L)-non phosphorylated 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 | 6.59 | 10.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.49 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 9.96 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.11 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 8.60 |
| CHEMBL386051 | — | — | 1 | 8.49 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 8.00 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.92 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.70 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.27 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.12 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.77 |
| CHEMBL1908396 | — | — | 1 | 6.47 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.44 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.41 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.35 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.32 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.24 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.21 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.19 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.14 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.11 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.08 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.04 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.03 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 5.89 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 5.85 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 5.82 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.82 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.64 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.032 | nM | 10.49 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 0.11 | nM | 9.96 |
| CHEMBL574738 | AST-487 | Kd | = | 0.77 | nM | 9.11 |
| CHEMBL941 | IMATINIB | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL386051 | — | Kd | = | 3.2 | nM | 8.49 |
| CHEMBL1908391 | MASITINIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL255863 | NILOTINIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL1230609 | FORETINIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL509032 | TAE-684 | Kd | = | 54.0 | nM | 7.27 |
| CHEMBL24828 | VANDETANIB | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL1908396 | — | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL1908397 | KW-2449 | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 450.0 | nM | 6.35 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 480.0 | nM | 6.32 |
| CHEMBL1173655 | AFATINIB | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 610.0 | nM | 6.21 |
| CHEMBL553 | ERLOTINIB | Kd | = | 640.0 | nM | 6.19 |
| CHEMBL535 | SUNITINIB | Kd | = | 730.0 | nM | 6.14 |
| CHEMBL1336 | SORAFENIB | Kd | = | 770.0 | nM | 6.11 |
| CHEMBL1289926 | AXITINIB | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL572881 | MOTESANIB | Kd | = | 910.0 | nM | 6.04 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 940.0 | nM | 6.03 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL31965 | CANERTINIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL558752 | RAF-265 | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL1908395 | — | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL939 | GEFITINIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL1721885 | SU-014813 | Kd | = | 3300.0 | nM | 5.48 |
| CHEMBL377300 | BRIVANIB | Kd | = | 4100.0 | nM | 5.39 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 4400.0 | nM | 5.36 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7600.0 | nM | 5.12 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |