Assay Detail
Binding
CHEMBL1787525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human KIT incubated for 1 hr by kinase binding assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 39 | 7.61 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.43 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.21 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 9.17 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.70 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.57 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 8.55 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 8.43 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 8.29 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.27 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.12 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.85 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 7.77 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.72 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.51 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 6.77 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.70 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.66 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.62 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.58 |
| CHEMBL191003 | JNJ-7706621 | — | 1 | 5.75 |
| CHEMBL1782075 | — | — | 1 | 5.66 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 5.11 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | - |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
| CHEMBL573339 | PI-103 | — | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL278041 | SB-202190 | — | 1 | - |
| CHEMBL10 | SB-203580 | — | 1 | - |
| CHEMBL440084 | SB-431542 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 0.37 | nM | 9.43 |
| CHEMBL5416410 | DASATINIB | Kd | = | 0.62 | nM | 9.21 |
| CHEMBL1721885 | SU-014813 | Kd | = | 0.68 | nM | 9.17 |
| CHEMBL223360 | LINIFANIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2.8 | nM | 8.55 |
| CHEMBL572881 | MOTESANIB | Kd | = | 3.7 | nM | 8.43 |
| CHEMBL101253 | VATALANIB | Kd | = | 5.1 | nM | 8.29 |
| CHEMBL574738 | AST-487 | Kd | = | 5.4 | nM | 8.27 |
| CHEMBL522892 | DOVITINIB | Kd | = | 7.5 | nM | 8.12 |
| CHEMBL941 | IMATINIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL1336 | SORAFENIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL558752 | RAF-265 | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL24828 | VANDETANIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL191003 | JNJ-7706621 | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1782075 | — | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | Kd | = | 7800.0 | nM | 5.11 |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 10000.0 | nM | - |
| CHEMBL607707 | PELITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL440084 | SB-431542 | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL278041 | SB-202190 | Kd | > | 10000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 10000.0 | nM | - |