Assay Detail
Binding
CHEMBL1787527
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human KIT D816V mutant 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 | 6.46 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.19 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.59 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.11 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.54 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.09 |
| CHEMBL1782075 | — | — | 1 | 6.96 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.54 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.54 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.51 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.47 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 6.44 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.42 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.39 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.30 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.09 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.04 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.85 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.80 |
| CHEMBL191003 | JNJ-7706621 | — | 1 | 5.60 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 5.41 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.37 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.34 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 5.34 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 5.21 |
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | - |
| CHEMBL440084 | SB-431542 | — | 1 | - |
| CHEMBL10 | SB-203580 | — | 1 | - |
| CHEMBL278041 | SB-202190 | — | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL573339 | PI-103 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 0.64 | nM | 9.19 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 7.7 | nM | 8.11 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL223360 | LINIFANIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL1782075 | — | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL24828 | VANDETANIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL1336 | SORAFENIB | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL1721885 | SU-014813 | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL574738 | AST-487 | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL535 | SUNITINIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL572881 | MOTESANIB | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL941 | IMATINIB | Kd | = | 820.0 | nM | 6.09 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 920.0 | nM | 6.04 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL191003 | JNJ-7706621 | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL939 | GEFITINIB | Kd | = | 4300.0 | nM | 5.37 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL558752 | RAF-265 | Kd | = | 6200.0 | nM | 5.21 |
| CHEMBL103667 | DORAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL101253 | VATALANIB | 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 | - |
| CHEMBL554 | LAPATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | 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 | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |