Assay Detail
Binding
CHEMBL1908681
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Binding constant for ABL1(H396P)-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 | 6.80 | 10.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.34 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 10.24 |
| CHEMBL386051 | — | — | 1 | 8.85 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.51 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.85 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.68 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 7.64 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.62 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.51 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.44 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.35 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.31 |
| CHEMBL1241674 | — | — | 1 | 7.24 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.24 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.24 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.22 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.21 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.19 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.06 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.96 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.85 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.85 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.80 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.41 |
| CHEMBL1908395 | — | — | 1 | 6.36 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.34 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.30 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.25 |
| CHEMBL1908396 | — | — | 1 | 6.21 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.046 | nM | 10.34 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 0.057 | nM | 10.24 |
| CHEMBL386051 | — | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL24828 | VANDETANIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL255863 | NILOTINIB | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL1289926 | AXITINIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL1908397 | KW-2449 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL574738 | AST-487 | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL31965 | CANERTINIB | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL553 | ERLOTINIB | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL1241674 | — | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL522892 | DOVITINIB | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 61.0 | nM | 7.21 |
| CHEMBL941 | IMATINIB | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 87.0 | nM | 7.06 |
| CHEMBL1230609 | FORETINIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL1908391 | MASITINIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL535 | SUNITINIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL509032 | TAE-684 | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL475251 | R-406 | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL1908395 | — | Kd | = | 440.0 | nM | 6.36 |
| CHEMBL939 | GEFITINIB | Kd | = | 460.0 | nM | 6.34 |
| CHEMBL1173655 | AFATINIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL1721885 | SU-014813 | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL1908396 | — | Kd | = | 620.0 | nM | 6.21 |
| CHEMBL377300 | BRIVANIB | Kd | = | 640.0 | nM | 6.19 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 700.0 | nM | 6.16 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 870.0 | nM | 6.06 |
| CHEMBL259084 | MLN-8054 | Kd | = | 940.0 | nM | 6.03 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL1336 | SORAFENIB | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL513909 | BI-2536 | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL230011 | TG100-115 | Kd | = | 3800.0 | nM | 5.42 |
| CHEMBL10 | SB-203580 | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 5600.0 | nM | 5.25 |
| CHEMBL558752 | RAF-265 | Kd | = | 5600.0 | nM | 5.25 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 6700.0 | nM | 5.17 |
| CHEMBL450786 | PHA-665752 | Kd | = | 9000.0 | nM | 5.05 |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |