Assay Detail
Binding
CHEMBL1908622
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for RIPK2 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
Receptor-interacting serine/threonine-protein kinase 2 (CHEMBL5014) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.14 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 8.34 |
| CHEMBL386051 | — | — | 1 | 7.80 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.68 |
| CHEMBL10 | SB-203580 | — | 1 | 7.62 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 7.51 |
| CHEMBL1241674 | — | — | 1 | 7.11 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.01 |
| CHEMBL1908396 | — | — | 1 | 6.54 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.52 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.37 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 6.30 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.28 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.24 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.19 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.17 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.05 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.02 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.01 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 5.96 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 5.89 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 5.75 |
| CHEMBL525191 | — | — | 1 | 5.60 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 5.57 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.57 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 5.54 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 5.44 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 5.43 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.43 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 5.28 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24828 | VANDETANIB | Kd | = | 4.6 | nM | 8.34 |
| CHEMBL386051 | — | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL1230609 | FORETINIB | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL10 | SB-203580 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL5416410 | DASATINIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL1241674 | — | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 98.0 | nM | 7.01 |
| CHEMBL1908396 | — | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL31965 | CANERTINIB | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL230011 | TG100-115 | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL939 | GEFITINIB | Kd | = | 530.0 | nM | 6.28 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 640.0 | nM | 6.19 |
| CHEMBL553 | ERLOTINIB | Kd | = | 680.0 | nM | 6.17 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 900.0 | nM | 6.05 |
| CHEMBL558752 | RAF-265 | Kd | = | 950.0 | nM | 6.02 |
| CHEMBL475251 | R-406 | Kd | = | 970.0 | nM | 6.01 |
| CHEMBL574738 | AST-487 | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1336 | SORAFENIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL525191 | — | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL1173655 | AFATINIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL377300 | BRIVANIB | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL554 | LAPATINIB | Kd | = | 3600.0 | nM | 5.44 |
| CHEMBL1908397 | KW-2449 | Kd | = | 3700.0 | nM | 5.43 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 3700.0 | nM | 5.43 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 5200.0 | nM | 5.28 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 5800.0 | nM | 5.24 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 6100.0 | nM | 5.21 |
| CHEMBL572881 | MOTESANIB | Kd | = | 9300.0 | nM | 5.03 |
| CHEMBL509032 | TAE-684 | Kd | = | 9600.0 | nM | 5.02 |
| CHEMBL1289926 | AXITINIB | Kd | = | 9900.0 | nM | 5.00 |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |