Assay Detail
Binding
CHEMBL1908687
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Binding constant for ABL1(Y253F)-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 | 6.91 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 10.44 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.24 |
| CHEMBL386051 | — | — | 1 | 9.06 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.11 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 8.05 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.00 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.89 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.64 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 7.60 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.44 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.43 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.43 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.38 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.34 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.26 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.25 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.13 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.12 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.00 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.89 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.85 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.64 |
| CHEMBL1908395 | — | — | 1 | 6.46 |
| CHEMBL1241674 | — | — | 1 | 6.46 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.44 |
| CHEMBL1908396 | — | — | 1 | 6.37 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.32 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.24 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.18 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288441 | BOSUTINIB | Kd | = | 0.036 | nM | 10.44 |
| CHEMBL5416410 | DASATINIB | Kd | = | 0.058 | nM | 10.24 |
| CHEMBL386051 | — | Kd | = | 0.88 | nM | 9.06 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 7.8 | nM | 8.11 |
| CHEMBL24828 | VANDETANIB | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL574738 | AST-487 | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL255863 | NILOTINIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL1908391 | MASITINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL1908397 | KW-2449 | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL1230609 | FORETINIB | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL31965 | CANERTINIB | Kd | = | 42.0 | nM | 7.38 |
| CHEMBL522892 | DOVITINIB | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 56.0 | nM | 7.25 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 74.0 | nM | 7.13 |
| CHEMBL553 | ERLOTINIB | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL509032 | TAE-684 | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL941 | IMATINIB | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL535 | SUNITINIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL1289926 | AXITINIB | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL1908395 | — | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL1241674 | — | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL939 | GEFITINIB | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL1908396 | — | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 480.0 | nM | 6.32 |
| CHEMBL1721885 | SU-014813 | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL1336 | SORAFENIB | Kd | = | 660.0 | nM | 6.18 |
| CHEMBL1173655 | AFATINIB | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 910.0 | nM | 6.04 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL450786 | PHA-665752 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL475251 | R-406 | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL558752 | RAF-265 | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 3800.0 | nM | 5.42 |
| CHEMBL572881 | MOTESANIB | Kd | = | 4500.0 | nM | 5.35 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 8500.0 | nM | 5.07 |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |