Assay Detail
Binding
CHEMBL4417038
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Inhibition of recombinant human N-terminal His-tagged MetAP2 (2 to 478 residues) using Met-Ala-Ser as substrate and MnCl2 as co-facor preincubated for 15 mins followed by substrate addition and measured after 45 mins by AAO/horse radish peroxidase enzyme coupled assay
26
Total Activities
26
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 |
Publication
Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.15 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454587 | — | — | 1 | 7.47 |
| CHEMBL4445117 | — | — | 1 | 7.39 |
| CHEMBL4551283 | — | — | 1 | 7.36 |
| CHEMBL4460950 | — | — | 1 | 7.28 |
| CHEMBL4547442 | — | — | 1 | 7.28 |
| CHEMBL4522216 | — | — | 1 | 7.28 |
| CHEMBL4464946 | — | — | 1 | 7.27 |
| CHEMBL4550096 | — | — | 1 | 7.24 |
| CHEMBL4463138 | — | — | 1 | 7.23 |
| CHEMBL4570368 | — | — | 1 | 7.21 |
| CHEMBL4448724 | — | — | 1 | 7.20 |
| CHEMBL4460444 | — | — | 1 | 7.19 |
| CHEMBL4448427 | — | — | 1 | 7.15 |
| CHEMBL4572028 | — | — | 1 | 7.13 |
| CHEMBL4475680 | — | — | 1 | 7.12 |
| CHEMBL4458906 | — | — | 1 | 7.10 |
| CHEMBL4450159 | — | — | 1 | 7.10 |
| CHEMBL4451402 | — | — | 1 | 7.06 |
| CHEMBL4591797 | — | — | 1 | 7.04 |
| CHEMBL4566917 | — | — | 1 | 7.03 |
| CHEMBL4441643 | — | — | 1 | 7.02 |
| CHEMBL4553094 | — | — | 1 | 7.00 |
| CHEMBL4470242 | — | — | 1 | 6.96 |
| CHEMBL4473359 | — | — | 1 | 6.96 |
| CHEMBL4444681 | — | — | 1 | 6.92 |
| CHEMBL4575412 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454587 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4445117 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4551283 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4460950 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4547442 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4522216 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4464946 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4550096 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4463138 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4570368 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4448724 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4460444 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4448427 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4572028 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4475680 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4458906 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4450159 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4451402 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4591797 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4566917 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4441643 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4553094 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4470242 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4473359 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4444681 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4575412 | — | IC50 | = | 160.0 | nM | 6.80 |