Assay Detail
Binding
CHEMBL5136367
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length wild type LRRK2 (unknown origin) using LRRKtide as substrate incubated for 1 hr in presence of ATP by TR-FRET based ADAPTA assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Leucine-rich repeat serine/threonine-protein kinase 2 (CHEMBL1075104) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 1<i>H-</i>Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.81 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | — | 1 | 9.00 |
| CHEMBL5177578 | — | — | 1 | 8.09 |
| CHEMBL5181966 | — | — | 1 | 7.77 |
| CHEMBL5170238 | — | — | 1 | 7.70 |
| CHEMBL5174380 | — | — | 1 | 7.59 |
| CHEMBL5173029 | — | — | 1 | 7.57 |
| CHEMBL5179102 | — | — | 1 | 7.40 |
| CHEMBL5198878 | — | — | 1 | 7.35 |
| CHEMBL5204372 | — | — | 1 | 7.33 |
| CHEMBL5198203 | — | — | 1 | 7.29 |
| CHEMBL5172291 | — | — | 1 | 7.20 |
| CHEMBL5170225 | — | — | 1 | 7.18 |
| CHEMBL5187306 | — | — | 1 | 7.17 |
| CHEMBL5190962 | — | — | 1 | 7.16 |
| CHEMBL5185136 | — | — | 1 | 7.14 |
| CHEMBL5185437 | — | — | 1 | 7.11 |
| CHEMBL5207639 | — | — | 1 | 7.05 |
| CHEMBL5199239 | — | — | 1 | 6.85 |
| CHEMBL5196289 | — | — | 1 | 6.76 |
| CHEMBL5197009 | — | — | 1 | 6.73 |
| CHEMBL5200500 | — | — | 1 | 6.71 |
| CHEMBL5199105 | — | — | 1 | 6.65 |
| CHEMBL5205363 | — | — | 1 | 6.61 |
| CHEMBL5202841 | — | — | 1 | 6.60 |
| CHEMBL5188336 | — | — | 1 | 6.58 |
| CHEMBL5190480 | — | — | 1 | 6.56 |
| CHEMBL5194234 | — | — | 1 | 6.56 |
| CHEMBL5191932 | — | — | 1 | 6.49 |
| CHEMBL5207757 | — | — | 1 | 6.47 |
| CHEMBL5198788 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5177578 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5181966 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL5170238 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL5174380 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL5173029 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL5179102 | — | IC50 | = | 40.2 | nM | 7.40 |
| CHEMBL5198878 | — | IC50 | = | 44.3 | nM | 7.35 |
| CHEMBL5204372 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL5198203 | — | IC50 | = | 51.4 | nM | 7.29 |
| CHEMBL5172291 | — | IC50 | = | 62.9 | nM | 7.20 |
| CHEMBL5170225 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5187306 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5190962 | — | IC50 | = | 69.7 | nM | 7.16 |
| CHEMBL5185136 | — | IC50 | = | 72.7 | nM | 7.14 |
| CHEMBL5185437 | — | IC50 | = | 77.6 | nM | 7.11 |
| CHEMBL5207639 | — | IC50 | = | 89.4 | nM | 7.05 |
| CHEMBL5199239 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5196289 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5197009 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL5200500 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL5199105 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL5205363 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL5202841 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL5188336 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5190480 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5194234 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5191932 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL5207757 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL5195211 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL5198788 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL5185379 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL5202898 | — | IC50 | = | 853.0 | nM | 6.07 |
| CHEMBL5173076 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL5207466 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL5183984 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL5198175 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL5208171 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL5184765 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL5170423 | — | IC50 | = | 2580.0 | nM | 5.59 |