Assay Detail
ADMET
CHEMBL4722525
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Inhibition of human MetAP1 expressed in Escherichia coli BL21 (DE3) using L-methionine-4-methyl-coumary1-7-amide as substrate preincubated for 30 mins followed by substrate addition and measured at 1 min interval for 30 mins by spectrofluorometric method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and characterization of quinoline-carbaldehyde derivatives as novel inhibitors for leishmanial methionine aminopeptidase 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.63 | 5.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740594 | — | — | 1 | 5.05 |
| CHEMBL4783117 | — | — | 1 | 4.96 |
| CHEMBL4758588 | — | — | 1 | 4.90 |
| CHEMBL4741746 | — | — | 1 | 4.21 |
| CHEMBL4743353 | — | — | 1 | 4.01 |
| CHEMBL4759464 | — | — | 1 | - |
| CHEMBL4764436 | — | — | 1 | - |
| CHEMBL4745980 | — | — | 1 | - |
| CHEMBL4749821 | — | — | 1 | - |
| CHEMBL4784882 | — | — | 1 | - |
| CHEMBL4743733 | — | — | 1 | - |
| CHEMBL4755128 | — | — | 1 | - |
| CHEMBL4795438 | — | — | 1 | - |
| CHEMBL4777085 | — | — | 1 | - |
| CHEMBL4785449 | — | — | 1 | - |
| CHEMBL4752621 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740594 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4783117 | — | IC50 | = | 10940.0 | nM | 4.96 |
| CHEMBL4758588 | — | IC50 | = | 12580.0 | nM | 4.90 |
| CHEMBL4741746 | — | IC50 | = | 61400.0 | nM | 4.21 |
| CHEMBL4743353 | — | IC50 | = | 98700.0 | nM | 4.01 |
| CHEMBL4759464 | — | IC50 | = | 126800.0 | nM | - |
| CHEMBL4764436 | — | IC50 | = | 174600.0 | nM | - |
| CHEMBL4745980 | — | IC50 | = | 112700.0 | nM | - |
| CHEMBL4749821 | — | IC50 | = | 104200.0 | nM | - |
| CHEMBL4784882 | — | IC50 | = | 127500.0 | nM | - |
| CHEMBL4743733 | — | IC50 | = | 284000.0 | nM | - |
| CHEMBL4755128 | — | IC50 | = | 217200.0 | nM | - |
| CHEMBL4795438 | — | IC50 | = | 107000.0 | nM | - |
| CHEMBL4777085 | — | IC50 | = | 116100.0 | nM | - |
| CHEMBL4785449 | — | IC50 | = | 143000.0 | nM | - |
| CHEMBL4752621 | — | IC50 | = | 104700.0 | nM | - |