Assay Detail
Binding
CHEMBL5683280
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Inhibition of LRRK2 G2019S mutant (unknown origin) using LRRKtide as substrate incubated for 1 hrs in presence of ATP by Adapta TR-FRET assay
22
Total Activities
22
Compounds Tested
1
Activity Types
2
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
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.02 | 8.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1673043 | — | — | 1 | 8.40 |
| CHEMBL2381339 | — | — | 1 | 8.30 |
| CHEMBL5686992 | — | — | 1 | 8.30 |
| CHEMBL1673048 | — | — | 1 | 8.10 |
| CHEMBL1673040 | — | — | 1 | 7.77 |
| CHEMBL1673039 | — | — | 1 | 7.58 |
| CHEMBL1673041 | — | — | 1 | 7.51 |
| CHEMBL1673051 | — | — | 1 | 7.28 |
| CHEMBL1673046 | — | — | 1 | 7.23 |
| CHEMBL5687018 | — | — | 1 | 7.21 |
| CHEMBL1673047 | — | — | 1 | 7.16 |
| CHEMBL1672987 | — | — | 1 | 7.04 |
| CHEMBL4632948 | — | — | 1 | 6.59 |
| CHEMBL2381340 | — | — | 1 | 6.47 |
| CHEMBL1673052 | — | — | 1 | 6.44 |
| CHEMBL5686989 | — | — | 1 | 6.36 |
| CHEMBL1673053 | — | — | 1 | 6.11 |
| CHEMBL1673057 | — | — | 1 | 5.97 |
| CHEMBL5687010 | — | — | 1 | 5.62 |
| CHEMBL1673056 | — | — | 1 | 5.00 |
| CHEMBL5687020 | — | — | 1 | - |
| CHEMBL5687005 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1673043 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2381339 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5686992 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1673048 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1673040 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1673039 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1673041 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1673051 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1673046 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5687018 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1673047 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1672987 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4632948 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL2381340 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL1673052 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5686989 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL1673053 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL1673057 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL5687010 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL1673056 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5687020 | — | IC50 | > | 493.0 | nM | - |
| CHEMBL5687005 | — | IC50 | > | 10000.0 | nM | - |