Assay Detail
Binding
CHEMBL3991920
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
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.51 | 9.15 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | no |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 9.15 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 7.50 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 7.42 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.55 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.40 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.99 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 5.92 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.85 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.73 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.62 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.46 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | - |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | - |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | - |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | - |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | - |
| CHEMBL2103882 | TIVANTINIB | 3.0 | 1 | - |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | - |
| CHEMBL1201182 | TEMSIROLIMUS | 4.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | - |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | - |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | - |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | - |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | - |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL495727 | AT-9283 | Kd | = | 279.0 | nM | 6.55 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 401.0 | nM | 6.40 |
| CHEMBL482967 | CYC-116 | Kd | = | 1021.0 | nM | 5.99 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 1196.0 | nM | 5.92 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1401.0 | nM | 5.85 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 1866.0 | nM | 5.73 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 2382.0 | nM | 5.62 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 3468.0 | nM | 5.46 |
| CHEMBL2017974 | BUPARLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2403108 | CERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL460702 | BMS-777607 | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1946170 | REGORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL1801204 | AZD-8055 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544983 | TESEVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL1079175 | MK-2206 | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL2364611 | GALUNISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |