Assay Detail
Binding
CHEMBL3991654
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 |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.42 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 8.52 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 8.10 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 7.89 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.50 |
| CHEMBL3688339 | — | — | 1 | 7.47 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 7.46 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 7.44 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.30 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 6.95 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 6.90 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.50 |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | 6.35 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.28 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.98 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.96 |
| CHEMBL3699142 | — | — | 1 | 5.96 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 5.93 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.92 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 5.76 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 5.70 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.63 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 5.57 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.56 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.51 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 5.47 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.43 |
| CHEMBL3991935 | — | — | 1 | 5.42 |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | 5.42 |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | - |
| CHEMBL3120215 | OSI-027 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545083 | RGB-286638 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL445813 | AT-7519 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL495727 | AT-9283 | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL3688339 | — | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL296468 | BMS-387032 | Kd | = | 113.0 | nM | 6.95 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 125.0 | nM | 6.90 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 314.0 | nM | 6.50 |
| CHEMBL1230607 | PHA-793887 | Kd | = | 444.0 | nM | 6.35 |
| CHEMBL564829 | MILCICLIB | Kd | = | 526.0 | nM | 6.28 |
| CHEMBL3545085 | XL-228 | Kd | = | 1055.0 | nM | 5.98 |
| CHEMBL3699142 | — | Kd | = | 1096.0 | nM | 5.96 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1092.0 | nM | 5.96 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 1162.0 | nM | 5.93 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 1213.0 | nM | 5.92 |
| CHEMBL1171837 | PONATINIB | Kd | = | 1729.0 | nM | 5.76 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 1994.0 | nM | 5.70 |
| CHEMBL535 | SUNITINIB | Kd | = | 2353.0 | nM | 5.63 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 2668.0 | nM | 5.57 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 2778.0 | nM | 5.56 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 3097.0 | nM | 5.51 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 3387.0 | nM | 5.47 |
| CHEMBL482967 | CYC-116 | Kd | = | 3714.0 | nM | 5.43 |
| CHEMBL3545110 | RIBOCICLIB | Kd | = | 3845.0 | nM | 5.42 |
| CHEMBL3991935 | — | Kd | = | 3762.0 | nM | 5.42 |
| CHEMBL460702 | BMS-777607 | Kd | > | 30000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544932 | TAK-901 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL3600873 | MK-5108 | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |