Assay Detail
Binding
CHEMBL4722526
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Inhibition of Leishmania donovani 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
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Leishmania donovani |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 20 | 4.66 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4743733 | — | — | 1 | 5.96 |
| CHEMBL4759563 | — | — | 1 | 5.88 |
| CHEMBL4740594 | — | — | 1 | 5.06 |
| CHEMBL4755128 | — | — | 1 | 4.93 |
| CHEMBL4741746 | — | — | 1 | 4.89 |
| CHEMBL4758588 | — | — | 1 | 4.74 |
| CHEMBL4743353 | — | — | 1 | 4.74 |
| CHEMBL4783117 | — | — | 1 | 4.58 |
| CHEMBL4759464 | — | — | 1 | 4.55 |
| CHEMBL4749821 | — | — | 1 | 4.43 |
| CHEMBL4764436 | — | — | 1 | 4.43 |
| CHEMBL4751907 | — | — | 1 | 4.40 |
| CHEMBL4784882 | — | — | 1 | 4.36 |
| CHEMBL4745980 | — | — | 1 | 4.34 |
| CHEMBL4785449 | — | — | 1 | 4.34 |
| CHEMBL4784127 | — | — | 1 | 4.33 |
| CHEMBL4795438 | — | — | 1 | 4.27 |
| CHEMBL4752621 | — | — | 1 | 4.20 |
| CHEMBL4777085 | — | — | 1 | 4.10 |
| CHEMBL4799662 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4743733 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4759563 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4740594 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4755128 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4741746 | — | IC50 | = | 12940.0 | nM | 4.89 |
| CHEMBL4758588 | — | IC50 | = | 18420.0 | nM | 4.74 |
| CHEMBL4743353 | — | IC50 | = | 18420.0 | nM | 4.74 |
| CHEMBL4783117 | — | IC50 | = | 26440.0 | nM | 4.58 |
| CHEMBL4759464 | — | IC50 | = | 27910.0 | nM | 4.55 |
| CHEMBL4749821 | — | IC50 | = | 36770.0 | nM | 4.43 |
| CHEMBL4764436 | — | IC50 | = | 37380.0 | nM | 4.43 |
| CHEMBL4751907 | — | IC50 | = | 39710.0 | nM | 4.40 |
| CHEMBL4784882 | — | IC50 | = | 43800.0 | nM | 4.36 |
| CHEMBL4745980 | — | IC50 | = | 46140.0 | nM | 4.34 |
| CHEMBL4785449 | — | IC50 | = | 45490.0 | nM | 4.34 |
| CHEMBL4784127 | — | IC50 | = | 46360.0 | nM | 4.33 |
| CHEMBL4795438 | — | IC50 | = | 54100.0 | nM | 4.27 |
| CHEMBL4752621 | — | IC50 | = | 62500.0 | nM | 4.20 |
| CHEMBL4777085 | — | IC50 | = | 79870.0 | nM | 4.10 |
| CHEMBL4799662 | — | IC50 | = | 251600.0 | nM | - |