Assay Detail
Binding
CHEMBL1908808
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Binding constant for RIOK2 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
Serine/threonine-protein kinase RIO2 (CHEMBL6000) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.02 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.31 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.01 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.85 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.60 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.58 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.41 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 6.26 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.21 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.17 |
| CHEMBL573339 | PI-103 | — | 1 | 6.11 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.11 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 5.92 |
| CHEMBL525191 | — | — | 1 | 5.92 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 5.82 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 5.82 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 5.77 |
| CHEMBL464552 | — | — | 1 | 5.70 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.58 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 5.47 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.30 |
| CHEMBL379218 | — | — | 1 | 5.28 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 5.17 |
| CHEMBL1241674 | — | — | 1 | 5.04 |
| CHEMBL249697 | BMS-345541 | — | 1 | - |
| CHEMBL10 | SB-203580 | — | 1 | - |
| CHEMBL608154 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 97.0 | nM | 7.01 |
| CHEMBL1721885 | SU-014813 | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL522892 | DOVITINIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL574738 | AST-487 | Kd | = | 550.0 | nM | 6.26 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 610.0 | nM | 6.21 |
| CHEMBL521851 | PICTILISIB | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 770.0 | nM | 6.11 |
| CHEMBL573339 | PI-103 | Kd | = | 770.0 | nM | 6.11 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL525191 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL296468 | BMS-387032 | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL230011 | TG100-115 | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL1908391 | MASITINIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL464552 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL475251 | R-406 | Kd | = | 3400.0 | nM | 5.47 |
| CHEMBL1908397 | KW-2449 | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL379218 | — | Kd | = | 5300.0 | nM | 5.28 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 6700.0 | nM | 5.17 |
| CHEMBL1241674 | — | Kd | = | 9100.0 | nM | 5.04 |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL386051 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL249697 | BMS-345541 | Kd | > | 10000.0 | nM | - |