Assay Detail
Binding
CHEMBL3991617
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
243
Total Activities
243
Compounds Tested
1
Activity Types
1
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K-562, COLO 205, SK-N-BE(2) and MV-4-11 |
| Subcellular | Cell lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
AarF domain-containing protein kinase 1 (CHEMBL4105885) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.27 | 7.64 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 7.64 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.62 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 7.48 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.40 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.82 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.70 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.66 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.64 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.55 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.26 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.25 |
| CHEMBL1236682 | REFAMETINIB | 2.0 | 1 | 6.11 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.97 |
| CHEMBL4084193 | — | — | 1 | 5.88 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 5.72 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 5.69 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.35 |
| CHEMBL281948 | K-252A | — | 1 | 5.21 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 4.79 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 4.64 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | - |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | - |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | - |
| CHEMBL1614766 | RO-4987655 | 1.0 | 1 | - |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | - |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | - |
| CHEMBL536151 | IMD-0354 | 1.0 | 1 | - |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL475251 | R-406 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 152.0 | nM | 6.82 |
| CHEMBL3545328 | XL-019 | Kd | = | 202.0 | nM | 6.70 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 217.0 | nM | 6.66 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 231.0 | nM | 6.64 |
| CHEMBL253969 | OSI-632 | Kd | = | 281.0 | nM | 6.55 |
| CHEMBL482967 | CYC-116 | Kd | = | 545.0 | nM | 6.26 |
| CHEMBL495727 | AT-9283 | Kd | = | 559.0 | nM | 6.25 |
| CHEMBL1236682 | REFAMETINIB | Kd | = | 778.0 | nM | 6.11 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 1071.0 | nM | 5.97 |
| CHEMBL4084193 | — | Kd | = | 1319.0 | nM | 5.88 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 1896.0 | nM | 5.72 |
| CHEMBL3301607 | FILGOTINIB | Kd | = | 2028.0 | nM | 5.69 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 4497.0 | nM | 5.35 |
| CHEMBL281948 | K-252A | Kd | = | 6090.0 | nM | 5.21 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 16218.0 | nM | 4.79 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 22747.0 | nM | 4.64 |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3039517 | RABUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3813873 | PEXIDARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1088752 | LOSMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL3544960 | AT-13148 | Kd | > | 30000.0 | nM | - |
| CHEMBL1738757 | REBASTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL2017974 | BUPARLISIB | Kd | > | 30000.0 | nM | - |