Assay Detail
Binding
CHEMBL1062839
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Binding constant for EGFR(L858R) kinase domain
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A quantitative analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 38 | 7.20 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 9.62 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 9.39 |
| 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 |
| CHEMBL483321 | CP-724714 | 2.0 | 1 | 6.96 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.92 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.57 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 6.40 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.12 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.01 |
| CHEMBL278041 | SB-202190 | — | 1 | 5.72 |
| CHEMBL10 | SB-203580 | — | 1 | 5.72 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 5.58 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 5.50 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL440084 | SB-431542 | — | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL191003 | JNJ-7706621 | — | 1 | - |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | - |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | - |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | - |
| CHEMBL573339 | PI-103 | — | 1 | - |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | - |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | Kd | = | 0.24 | nM | 9.62 |
| CHEMBL607707 | PELITINIB | Kd | = | 0.41 | nM | 9.39 |
| 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 |
| CHEMBL483321 | CP-724714 | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL5416410 | DASATINIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 760.0 | nM | 6.12 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 980.0 | nM | 6.01 |
| CHEMBL10 | SB-203580 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL278041 | SB-202190 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL574738 | AST-487 | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL259084 | MLN-8054 | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL103667 | DORAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 10000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL191003 | JNJ-7706621 | Kd | > | 10000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL440084 | SB-431542 | Kd | > | 10000.0 | nM | - |
| CHEMBL535 | SUNITINIB | Kd | > | 10000.0 | nM | - |