Assay Detail
Binding
CHEMBL1908700
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Binding constant for EGFR(L858R) 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 | 6.70 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.70 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 9.62 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 9.17 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.03 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 9.01 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.55 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 8.06 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.64 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.34 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.92 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.85 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.72 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.60 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.57 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 6.40 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.12 |
| CHEMBL386051 | — | — | 1 | 6.07 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.07 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.01 |
| CHEMBL1241674 | — | — | 1 | 6.00 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 5.89 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 5.85 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.77 |
| CHEMBL10 | SB-203580 | — | 1 | 5.72 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 5.58 |
| CHEMBL464552 | — | — | 1 | 5.54 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 5.50 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.48 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 5.29 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL31965 | CANERTINIB | Kd | = | 0.24 | nM | 9.62 |
| CHEMBL180022 | NERATINIB | Kd | = | 0.67 | nM | 9.17 |
| CHEMBL939 | GEFITINIB | Kd | = | 0.94 | nM | 9.03 |
| CHEMBL553 | ERLOTINIB | Kd | = | 0.97 | nM | 9.01 |
| CHEMBL554 | LAPATINIB | Kd | = | 2.8 | nM | 8.55 |
| CHEMBL24828 | VANDETANIB | Kd | = | 8.7 | nM | 8.06 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL509032 | TAE-684 | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL5416410 | DASATINIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL1230609 | FORETINIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL475251 | R-406 | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 760.0 | nM | 6.12 |
| CHEMBL386051 | — | Kd | = | 860.0 | nM | 6.07 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 860.0 | nM | 6.07 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 980.0 | nM | 6.01 |
| CHEMBL1241674 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL513909 | BI-2536 | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL230011 | TG100-115 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL10 | SB-203580 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL574738 | AST-487 | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL464552 | — | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL259084 | MLN-8054 | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 3300.0 | nM | 5.48 |
| CHEMBL377300 | BRIVANIB | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL572881 | MOTESANIB | Kd | = | 7100.0 | nM | 5.15 |
| CHEMBL1614701 | SELUMETINIB | Kd | = | 8000.0 | nM | 5.10 |
| CHEMBL384304 | RG-547 | Kd | = | 9100.0 | nM | 5.04 |
| CHEMBL502835 | NINTEDANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908395 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL249697 | BMS-345541 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 10000.0 | nM | - |