Assay Detail
Functional
CHEMBL896510
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Inhibition of Eg5 assessed as inhibition ATP hydrolysis by ATPase assay
25
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.66 | 6.82 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392369 | — | — | 2 | 6.82 |
| CHEMBL232133 | — | — | 2 | 6.66 |
| CHEMBL400633 | — | — | 2 | 6.17 |
| CHEMBL392695 | S-TRITYL-L-CYSTEINE | — | 2 | 5.75 |
| CHEMBL232121 | — | — | 1 | 5.51 |
| CHEMBL232728 | — | — | 1 | 5.24 |
| CHEMBL231939 | — | — | 1 | 4.83 |
| CHEMBL396414 | — | — | 1 | 4.26 |
| CHEMBL415259 | — | — | 1 | - |
| CHEMBL232727 | — | — | 1 | - |
| CHEMBL398146 | — | — | 1 | - |
| CHEMBL394875 | — | — | 1 | - |
| CHEMBL231992 | — | — | 1 | - |
| CHEMBL63130 | BENZYLCYSTEINE | — | 1 | - |
| CHEMBL302212 | — | — | 1 | - |
| CHEMBL396416 | CARBOCYSTEINE | 3.0 | 1 | - |
| CHEMBL397565 | — | — | 1 | - |
| CHEMBL392255 | — | — | 1 | - |
| CHEMBL863 | CYSTEINE | 4.0 | 1 | - |
| CHEMBL433998 | — | — | 1 | - |
| CHEMBL233547 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392369 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL232133 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL400633 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL392695 | S-TRITYL-L-CYSTEINE | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL232121 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL232728 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL231939 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL396414 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL400633 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL232133 | — | Inhibition | = | 79.0 | % | - |
| CHEMBL392695 | S-TRITYL-L-CYSTEINE | Inhibition | = | 89.0 | % | - |
| CHEMBL392369 | — | Inhibition | = | 98.0 | % | - |
| CHEMBL433998 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL863 | CYSTEINE | IC50 | > | 63000.0 | nM | - |
| CHEMBL392255 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL397565 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL396416 | CARBOCYSTEINE | IC50 | > | 63000.0 | nM | - |
| CHEMBL233547 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL63130 | BENZYLCYSTEINE | IC50 | > | 63000.0 | nM | - |
| CHEMBL231992 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL394875 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL398146 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL232727 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL415259 | — | IC50 | > | 63000.0 | nM | - |
| CHEMBL302212 | — | IC50 | > | 63000.0 | nM | - |