Assay Detail
Binding
CHEMBL5136368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length LRRK2 G2019S mutant (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 | 7.66 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | — | 1 | 9.40 |
| CHEMBL5177578 | — | — | 1 | 8.96 |
| CHEMBL5170238 | — | — | 1 | 8.66 |
| CHEMBL5181966 | — | — | 1 | 8.62 |
| CHEMBL5173029 | — | — | 1 | 8.54 |
| CHEMBL5174380 | — | — | 1 | 8.51 |
| CHEMBL5179102 | — | — | 1 | 8.40 |
| CHEMBL5172291 | — | — | 1 | 8.37 |
| CHEMBL5198878 | — | — | 1 | 8.21 |
| CHEMBL5185437 | — | — | 1 | 8.21 |
| CHEMBL5187306 | — | — | 1 | 8.21 |
| CHEMBL5204372 | — | — | 1 | 8.16 |
| CHEMBL5170225 | — | — | 1 | 8.12 |
| CHEMBL5207639 | — | — | 1 | 8.09 |
| CHEMBL5190962 | — | — | 1 | 8.06 |
| CHEMBL5198203 | — | — | 1 | 7.84 |
| CHEMBL5185136 | — | — | 1 | 7.82 |
| CHEMBL5202841 | — | — | 1 | 7.81 |
| CHEMBL5194234 | — | — | 1 | 7.78 |
| CHEMBL5200500 | — | — | 1 | 7.72 |
| CHEMBL5199239 | — | — | 1 | 7.71 |
| CHEMBL5196289 | — | — | 1 | 7.67 |
| CHEMBL5205363 | — | — | 1 | 7.61 |
| CHEMBL5197009 | — | — | 1 | 7.48 |
| CHEMBL5190480 | — | — | 1 | 7.46 |
| CHEMBL5188336 | — | — | 1 | 7.30 |
| CHEMBL5198175 | — | — | 1 | 7.24 |
| CHEMBL5199105 | — | — | 1 | 7.21 |
| CHEMBL5191932 | — | — | 1 | 7.12 |
| CHEMBL5202898 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5177578 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5170238 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5181966 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5173029 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5174380 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5179102 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5172291 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5198878 | — | IC50 | = | 6.15 | nM | 8.21 |
| CHEMBL5185437 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5187306 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5204372 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5170225 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5207639 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5190962 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5198203 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5185136 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL5202841 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5194234 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL5200500 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL5199239 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL5196289 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL5205363 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL5197009 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL5190480 | — | IC50 | = | 34.7 | nM | 7.46 |
| CHEMBL5188336 | — | IC50 | = | 49.9 | nM | 7.30 |
| CHEMBL5198175 | — | IC50 | = | 57.1 | nM | 7.24 |
| CHEMBL5199105 | — | IC50 | = | 61.4 | nM | 7.21 |
| CHEMBL5191932 | — | IC50 | = | 76.2 | nM | 7.12 |
| CHEMBL5202898 | — | IC50 | = | 87.8 | nM | 7.06 |
| CHEMBL5198788 | — | IC50 | = | 95.7 | nM | 7.02 |
| CHEMBL5207757 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5183984 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5195211 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5173076 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL5185379 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL5207466 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL5184765 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL5170423 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL5208171 | — | IC50 | = | 666.0 | nM | 6.18 |