Assay Detail
Binding
CHEMBL1908710
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Binding constant for LCK 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 | 6.75 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.70 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 9.23 |
| CHEMBL386051 | — | — | 1 | 8.96 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.22 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.21 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.96 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.77 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.52 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.52 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.52 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 7.51 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.40 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.33 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.31 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.21 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.17 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.14 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.92 |
| CHEMBL1908395 | — | — | 1 | 6.75 |
| CHEMBL1241674 | — | — | 1 | 6.70 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.64 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.60 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.60 |
| CHEMBL1908396 | — | — | 1 | 6.58 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.55 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.50 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.50 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.44 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.42 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 0.59 | nM | 9.23 |
| CHEMBL386051 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL1230609 | FORETINIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 6.2 | nM | 8.21 |
| CHEMBL574738 | AST-487 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL24828 | VANDETANIB | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL475251 | R-406 | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL1908391 | MASITINIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL941 | IMATINIB | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL255863 | NILOTINIB | Kd | = | 47.0 | nM | 7.33 |
| CHEMBL509032 | TAE-684 | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 61.0 | nM | 7.21 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL180022 | NERATINIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL1908395 | — | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL1241674 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL535 | SUNITINIB | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL522892 | DOVITINIB | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL553 | ERLOTINIB | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL1908396 | — | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL450786 | PHA-665752 | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL31965 | CANERTINIB | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL572881 | MOTESANIB | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 460.0 | nM | 6.34 |
| CHEMBL1173655 | AFATINIB | Kd | = | 570.0 | nM | 6.24 |
| CHEMBL259084 | MLN-8054 | Kd | = | 590.0 | nM | 6.23 |
| CHEMBL939 | GEFITINIB | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL558752 | RAF-265 | Kd | = | 640.0 | nM | 6.19 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1721885 | SU-014813 | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL1336 | SORAFENIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL1289926 | AXITINIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL10 | SB-203580 | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL230011 | TG100-115 | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 7200.0 | nM | 5.14 |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |