Assay Detail
Binding
CHEMBL1908675
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for ABL1(E255K)-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 | 6.90 | 10.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.33 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 10.33 |
| CHEMBL386051 | — | — | 1 | 9.26 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.52 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.89 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.66 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.52 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.44 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.44 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.40 |
| CHEMBL1241674 | — | — | 1 | 7.25 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.20 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.20 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 7.20 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.19 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.12 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.12 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.85 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.82 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.77 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.77 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.75 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.72 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.66 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.51 |
| CHEMBL1908395 | — | — | 1 | 6.43 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.40 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.38 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 6.24 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.047 | nM | 10.33 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 0.047 | nM | 10.33 |
| CHEMBL386051 | — | Kd | = | 0.55 | nM | 9.26 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL24828 | VANDETANIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL31965 | CANERTINIB | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL1908397 | KW-2449 | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL255863 | NILOTINIB | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL1241674 | — | Kd | = | 56.0 | nM | 7.25 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL553 | ERLOTINIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL1289926 | AXITINIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL574738 | AST-487 | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL522892 | DOVITINIB | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL1908391 | MASITINIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL1230609 | FORETINIB | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL941 | IMATINIB | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL535 | SUNITINIB | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL509032 | TAE-684 | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL475251 | R-406 | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL1721885 | SU-014813 | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL1908395 | — | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL939 | GEFITINIB | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL1173655 | AFATINIB | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL377300 | BRIVANIB | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL450786 | PHA-665752 | Kd | = | 770.0 | nM | 6.11 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 800.0 | nM | 6.10 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 840.0 | nM | 6.08 |
| CHEMBL1908396 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL1336 | SORAFENIB | Kd | = | 3400.0 | nM | 5.47 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 4500.0 | nM | 5.35 |
| CHEMBL513909 | BI-2536 | Kd | = | 5900.0 | nM | 5.23 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 9600.0 | nM | 5.02 |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |