Assay Detail
Binding
CHEMBL1061901
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Binding constant for KIT(V559D,V654A) 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 |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A quantitative analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 38 | 7.23 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.68 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 9.60 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.57 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.51 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.68 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 7.64 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.58 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.52 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.42 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.15 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.00 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.68 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.62 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.32 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.25 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.07 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.80 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 5.64 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 5.62 |
| CHEMBL483321 | CP-724714 | 2.0 | 1 | - |
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | - |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | - |
| CHEMBL440084 | SB-431542 | — | 1 | - |
| CHEMBL10 | SB-203580 | — | 1 | - |
| CHEMBL278041 | SB-202190 | — | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL573339 | PI-103 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 0.21 | nM | 9.68 |
| CHEMBL1721885 | SU-014813 | Kd | = | 0.25 | nM | 9.60 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL522892 | DOVITINIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL223360 | LINIFANIB | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL572881 | MOTESANIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL941 | IMATINIB | Kd | = | 71.0 | nM | 7.15 |
| CHEMBL574738 | AST-487 | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL101253 | VATALANIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL1336 | SORAFENIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 480.0 | nM | 6.32 |
| CHEMBL24828 | VANDETANIB | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL558752 | RAF-265 | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL191003 | JNJ-7706621 | Kd | > | 10000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL607707 | PELITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 10000.0 | nM | - |
| CHEMBL278041 | SB-202190 | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL440084 | SB-431542 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 10000.0 | nM | - |