Assay Detail
Binding
CHEMBL1908493
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Binding constant for MET(Y1235D) 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 | 6.28 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 9.09 |
| CHEMBL450786 | PHA-665752 | — | 1 | 9.08 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.82 |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | 8.41 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.39 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.85 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.75 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.44 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.34 |
| CHEMBL1908396 | — | — | 1 | 6.25 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.25 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.25 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.24 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 6.13 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.12 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.08 |
| CHEMBL386051 | — | — | 1 | 6.07 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.00 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.96 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 5.85 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 5.68 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.58 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 5.58 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 5.51 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.46 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 5.39 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 5.38 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.33 |
| CHEMBL1908395 | — | — | 1 | 5.27 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230609 | FORETINIB | Kd | = | 0.82 | nM | 9.09 |
| CHEMBL450786 | PHA-665752 | Kd | = | 0.83 | nM | 9.08 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL1236107 | SGX-523 | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL509032 | TAE-684 | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 460.0 | nM | 6.34 |
| CHEMBL1908396 | — | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL1908397 | KW-2449 | Kd | = | 570.0 | nM | 6.24 |
| CHEMBL574738 | AST-487 | Kd | = | 740.0 | nM | 6.13 |
| CHEMBL475251 | R-406 | Kd | = | 760.0 | nM | 6.12 |
| CHEMBL31965 | CANERTINIB | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL386051 | — | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL1289926 | AXITINIB | Kd | = | 990.0 | nM | 6.00 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL558752 | RAF-265 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2100.0 | nM | 5.68 |
| CHEMBL1173655 | AFATINIB | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL223360 | LINIFANIB | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL939 | GEFITINIB | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL24828 | VANDETANIB | Kd | = | 4100.0 | nM | 5.39 |
| CHEMBL180022 | NERATINIB | Kd | = | 4200.0 | nM | 5.38 |
| CHEMBL535 | SUNITINIB | Kd | = | 4700.0 | nM | 5.33 |
| CHEMBL1908395 | — | Kd | = | 5400.0 | nM | 5.27 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 5700.0 | nM | 5.24 |
| CHEMBL10 | SB-203580 | Kd | = | 7900.0 | nM | 5.10 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 8400.0 | nM | 5.08 |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL103667 | DORAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |