Assay Detail
Binding
CHEMBL4397057
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-tagged MetAP2 (2 to 478 residues) using Met-Ala-Ser as substrate and manganese as co-facor preincubated for 15 mins followed by substrate addition and measured after 45 mins by AAO/horse radish peroxidase enzyme coupled assay
35
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.67 | 7.30 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4566670 | — | — | 1 | 7.30 |
| CHEMBL4524329 | — | — | 1 | 7.30 |
| CHEMBL4438796 | — | — | 1 | 7.24 |
| CHEMBL4536649 | — | — | 1 | 7.22 |
| CHEMBL4460784 | — | — | 1 | 7.22 |
| CHEMBL4552396 | — | — | 1 | 7.22 |
| CHEMBL4462995 | — | — | 1 | 7.22 |
| CHEMBL4475680 | — | — | 1 | 7.13 |
| CHEMBL4466601 | — | — | 1 | 7.10 |
| CHEMBL4464652 | — | — | 1 | 7.10 |
| CHEMBL4558399 | — | — | 1 | 7.10 |
| CHEMBL4469817 | — | — | 1 | 7.05 |
| CHEMBL4465025 | — | — | 1 | 7.05 |
| CHEMBL4546986 | — | — | 1 | 7.05 |
| CHEMBL4559822 | — | — | 1 | 6.89 |
| CHEMBL4441859 | — | — | 1 | 6.85 |
| CHEMBL4584721 | — | — | 1 | 6.85 |
| CHEMBL4441472 | — | — | 1 | 6.77 |
| CHEMBL4463329 | — | — | 1 | 6.66 |
| CHEMBL4549484 | — | — | 1 | 6.62 |
| CHEMBL4589384 | — | — | 1 | 6.57 |
| CHEMBL4556036 | — | — | 1 | 6.55 |
| CHEMBL4447796 | — | — | 1 | 6.42 |
| CHEMBL4543409 | — | — | 1 | 6.39 |
| CHEMBL4464827 | — | — | 1 | 6.36 |
| CHEMBL4469283 | — | — | 1 | 6.32 |
| CHEMBL4576078 | — | — | 1 | 6.27 |
| CHEMBL4587873 | — | — | 1 | 6.26 |
| CHEMBL4444678 | — | — | 1 | 6.23 |
| CHEMBL4545625 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4566670 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4524329 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4438796 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4536649 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4460784 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4552396 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4462995 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4475680 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4466601 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4464652 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4558399 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4469817 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4465025 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4546986 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4559822 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4441859 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4584721 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4441472 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4463329 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4549484 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4589384 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4556036 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4447796 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4543409 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4464827 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4469283 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4576078 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4587873 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4444678 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4545625 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4563305 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4529723 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4556838 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4572185 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4568227 | — | Inhibition | - | % | - |