Assay Detail
Binding
CHEMBL1908438
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for LRRK2(G2019S) 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
Leucine-rich repeat serine/threonine-protein kinase 2 (CHEMBL1075104) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.61 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.41 |
| CHEMBL509032 | TAE-684 | — | 1 | 9.07 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.60 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.57 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.43 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.35 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 7.16 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.12 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.05 |
| CHEMBL464552 | — | — | 1 | 6.77 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.75 |
| CHEMBL1908395 | — | — | 1 | 6.43 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.26 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.08 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.06 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.00 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.00 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 5.96 |
| CHEMBL379218 | — | — | 1 | 5.85 |
| CHEMBL1241674 | — | — | 1 | 5.77 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.70 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 5.36 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.32 |
| CHEMBL386051 | — | — | 1 | 5.29 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 5.01 |
| CHEMBL608154 | — | — | 1 | - |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 0.39 | nM | 9.41 |
| CHEMBL509032 | TAE-684 | Kd | = | 0.86 | nM | 9.07 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL475251 | R-406 | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL1908397 | KW-2449 | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL1721885 | SU-014813 | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL535 | SUNITINIB | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL464552 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL1908395 | — | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 550.0 | nM | 6.26 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL522892 | DOVITINIB | Kd | = | 880.0 | nM | 6.06 |
| CHEMBL1289926 | AXITINIB | Kd | = | 990.0 | nM | 6.00 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL31965 | CANERTINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL379218 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL1241674 | — | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL574738 | AST-487 | Kd | = | 4400.0 | nM | 5.36 |
| CHEMBL553 | ERLOTINIB | Kd | = | 4800.0 | nM | 5.32 |
| CHEMBL386051 | — | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 9700.0 | nM | 5.01 |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1230020 | PLX-4720 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL450786 | PHA-665752 | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL608154 | — | Kd | > | 10000.0 | nM | - |