Assay Detail
Binding
CHEMBL1908481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for INSR 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 | 6.54 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464552 | — | — | 1 | 8.77 |
| CHEMBL509032 | TAE-684 | — | 1 | 8.62 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.62 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.96 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.68 |
| CHEMBL1908395 | — | — | 1 | 6.48 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.47 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.40 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.30 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.20 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.07 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 5.96 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 5.96 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.92 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 5.66 |
| CHEMBL450786 | PHA-665752 | — | 1 | 5.64 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 5.52 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL608154 | — | — | 1 | - |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | - |
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | - |
| CHEMBL386051 | — | — | 1 | - |
| CHEMBL10 | SB-203580 | — | 1 | - |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | - |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | - |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | - |
| CHEMBL261849 | GW632580X | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464552 | — | Kd | = | 1.7 | nM | 8.77 |
| CHEMBL509032 | TAE-684 | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL1230609 | FORETINIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL1908395 | — | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL1908397 | KW-2449 | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL535 | SUNITINIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL475251 | R-406 | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1721885 | SU-014813 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL574738 | AST-487 | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL450786 | PHA-665752 | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL180022 | NERATINIB | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL5416410 | DASATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL1789941 | RUXOLITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL24828 | VANDETANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL386051 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |