Assay Detail
Binding
CHEMBL1908683
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Binding constant for ABL1(Q252H)-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 | 7.04 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.43 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 10.07 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.03 |
| CHEMBL386051 | — | — | 1 | 8.89 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 8.74 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.42 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.40 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 8.22 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.00 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.75 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.68 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.41 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.33 |
| CHEMBL1908396 | — | — | 1 | 7.19 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.14 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.12 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.04 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.01 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.00 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.96 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.89 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.70 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.64 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.62 |
| CHEMBL1241674 | — | — | 1 | 6.62 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.54 |
| CHEMBL1908395 | — | — | 1 | 6.47 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.36 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.28 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.037 | nM | 10.43 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 0.086 | nM | 10.07 |
| CHEMBL574738 | AST-487 | Kd | = | 0.93 | nM | 9.03 |
| CHEMBL386051 | — | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL941 | IMATINIB | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 3.8 | nM | 8.42 |
| CHEMBL1230609 | FORETINIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL1908391 | MASITINIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL255863 | NILOTINIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL24828 | VANDETANIB | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL509032 | TAE-684 | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL1908397 | KW-2449 | Kd | = | 47.0 | nM | 7.33 |
| CHEMBL1908396 | — | Kd | = | 64.0 | nM | 7.19 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL522892 | DOVITINIB | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL31965 | CANERTINIB | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 97.0 | nM | 7.01 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL1336 | SORAFENIB | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL553 | ERLOTINIB | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL535 | SUNITINIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL1241674 | — | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL1289926 | AXITINIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL1908395 | — | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL558752 | RAF-265 | Kd | = | 440.0 | nM | 6.36 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 530.0 | nM | 6.28 |
| CHEMBL259084 | MLN-8054 | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL475251 | R-406 | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL572881 | MOTESANIB | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL1173655 | AFATINIB | Kd | = | 790.0 | nM | 6.10 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 860.0 | nM | 6.07 |
| CHEMBL1721885 | SU-014813 | Kd | = | 870.0 | nM | 6.06 |
| CHEMBL939 | GEFITINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL180022 | NERATINIB | Kd | = | 7100.0 | nM | 5.15 |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |