Assay Detail
Binding
CHEMBL1908654
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Binding constant for EPHB6 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 | 6.59 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.41 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.89 |
| CHEMBL386051 | — | — | 1 | 8.70 |
| CHEMBL1908396 | — | — | 1 | 8.30 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.22 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.55 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.48 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 7.37 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 7.30 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.12 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.09 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.01 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.89 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.85 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.68 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.66 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.66 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.62 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.52 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.51 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.46 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.44 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.30 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.19 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.07 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.00 |
| CHEMBL1908395 | — | — | 1 | 5.96 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.92 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 5.92 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.039 | nM | 10.41 |
| CHEMBL1230609 | FORETINIB | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL386051 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL1908396 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL223360 | LINIFANIB | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL558752 | RAF-265 | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL24828 | VANDETANIB | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 98.0 | nM | 7.01 |
| CHEMBL1908397 | KW-2449 | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL522892 | DOVITINIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL1336 | SORAFENIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL475251 | R-406 | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL509032 | TAE-684 | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL1289926 | AXITINIB | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL255863 | NILOTINIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL31965 | CANERTINIB | Kd | = | 640.0 | nM | 6.19 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 860.0 | nM | 6.07 |
| CHEMBL535 | SUNITINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL1908395 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1721885 | SU-014813 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL521851 | PICTILISIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL180022 | NERATINIB | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL450786 | PHA-665752 | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL1173655 | AFATINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL10 | SB-203580 | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL939 | GEFITINIB | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL1241674 | — | Kd | = | 9000.0 | nM | 5.05 |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |