Assay Detail
Binding
CHEMBL1908609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for TYK2(JH1domain-catalytic) kinase domain
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.65 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 9.05 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.32 |
| CHEMBL1908395 | — | — | 1 | 8.24 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.82 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.68 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.43 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.25 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.11 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.82 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.80 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 6.75 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.72 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.68 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.60 |
| CHEMBL1241674 | — | — | 1 | 6.55 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.39 |
| CHEMBL386051 | — | — | 1 | 6.37 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.29 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.80 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.75 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 5.75 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 5.47 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.44 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 5.30 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.29 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 5.19 |
| CHEMBL105442 | CI-1040 | 2.0 | 1 | - |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 0.9 | nM | 9.05 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 4.8 | nM | 8.32 |
| CHEMBL1908395 | — | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 56.0 | nM | 7.25 |
| CHEMBL509032 | TAE-684 | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL522892 | DOVITINIB | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL1908397 | KW-2449 | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL475251 | R-406 | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL1241674 | — | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL558752 | RAF-265 | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL386051 | — | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 510.0 | nM | 6.29 |
| CHEMBL535 | SUNITINIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL574738 | AST-487 | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 3400.0 | nM | 5.47 |
| CHEMBL1289926 | AXITINIB | Kd | = | 3600.0 | nM | 5.44 |
| CHEMBL1230609 | FORETINIB | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL1721885 | SU-014813 | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 6500.0 | nM | 5.19 |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL450786 | PHA-665752 | Kd | > | 10000.0 | nM | - |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 10000.0 | nM | - |