Assay Detail
Binding
CHEMBL1908538
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Binding constant for BLK 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 | 6.70 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.68 |
| CHEMBL386051 | — | — | 1 | 8.82 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.48 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.27 |
| CHEMBL1908395 | — | — | 1 | 7.96 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.82 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.60 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.52 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.35 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.19 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.18 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 7.17 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.07 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.96 |
| CHEMBL1908396 | — | — | 1 | 6.92 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.92 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.89 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.82 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.80 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.72 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.72 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.66 |
| CHEMBL1241674 | — | — | 1 | 6.62 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.42 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.30 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.30 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.28 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.19 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 6.17 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.21 | nM | 9.68 |
| CHEMBL386051 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL1230609 | FORETINIB | Kd | = | 5.4 | nM | 8.27 |
| CHEMBL1908395 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL475251 | R-406 | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL574738 | AST-487 | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL31965 | CANERTINIB | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL535 | SUNITINIB | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL24828 | VANDETANIB | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL259084 | MLN-8054 | Kd | = | 68.0 | nM | 7.17 |
| CHEMBL180022 | NERATINIB | Kd | = | 85.0 | nM | 7.07 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL1908396 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL509032 | TAE-684 | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL1908391 | MASITINIB | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL553 | ERLOTINIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL522892 | DOVITINIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL1173655 | AFATINIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL1241674 | — | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL255863 | NILOTINIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL941 | IMATINIB | Kd | = | 520.0 | nM | 6.28 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 650.0 | nM | 6.19 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 680.0 | nM | 6.17 |
| CHEMBL1721885 | SU-014813 | Kd | = | 750.0 | nM | 6.12 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL939 | GEFITINIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL450786 | PHA-665752 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL377300 | BRIVANIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL572881 | MOTESANIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL1289926 | AXITINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL1908397 | KW-2449 | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL558752 | RAF-265 | Kd | = | 7900.0 | nM | 5.10 |
| CHEMBL554 | LAPATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1789941 | RUXOLITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 10000.0 | nM | - |