Assay Detail
Binding
CHEMBL1908714
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Binding constant for TIE1 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 |
Target
Tyrosine-protein kinase receptor Tie-1 (CHEMBL5274) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.47 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.54 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 9.10 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 8.08 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.82 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.19 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.17 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.12 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 7.01 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 6.96 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.96 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.82 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.57 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.54 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.52 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.46 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.41 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.17 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.16 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.16 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.07 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.00 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 5.96 |
| CHEMBL386051 | — | — | 1 | 5.92 |
| CHEMBL450786 | PHA-665752 | — | 1 | 5.92 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.85 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 5.85 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 5.82 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 5.80 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 5.66 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL574738 | AST-487 | Kd | = | 0.29 | nM | 9.54 |
| CHEMBL1230609 | FORETINIB | Kd | = | 0.79 | nM | 9.10 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 8.3 | nM | 8.08 |
| CHEMBL509032 | TAE-684 | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL1336 | SORAFENIB | Kd | = | 68.0 | nM | 7.17 |
| CHEMBL475251 | R-406 | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL1289926 | AXITINIB | Kd | = | 97.0 | nM | 7.01 |
| CHEMBL223360 | LINIFANIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL558752 | RAF-265 | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL1908397 | KW-2449 | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL180022 | NERATINIB | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 680.0 | nM | 6.17 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 700.0 | nM | 6.16 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 700.0 | nM | 6.16 |
| CHEMBL553 | ERLOTINIB | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL255863 | NILOTINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL386051 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL450786 | PHA-665752 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL31965 | CANERTINIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL535 | SUNITINIB | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL522892 | DOVITINIB | Kd | = | 4000.0 | nM | 5.40 |
| CHEMBL1721885 | SU-014813 | Kd | = | 5700.0 | nM | 5.24 |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |