Assay Detail
Binding
CHEMBL1100258
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Inhibition of Trypanosoma cruzi trans-sialidase containing catalytic domain (N58F, R200K) and lectin-like domain (S495 K, V496G, E520K, D593G, I597D, H599R) mutation expressed in Escherichia coli JM109 assessed as MuNANA substrate hydrolysis in presence of 0.1% Triton X-100 by discontinuous fluorimetric assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma cruzi |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.62 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1089732 | — | — | 1 | 6.24 |
| CHEMBL418068 | RHEIN | — | 1 | 4.85 |
| CHEMBL164 | MYRICETIN | — | 1 | 4.77 |
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 4.66 |
| CHEMBL247484 | TRICETIN | — | 1 | 4.41 |
| CHEMBL55415 | SCUTELLAREIN | — | 1 | 4.30 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 4.24 |
| CHEMBL28 | APIGENIN | — | 1 | 4.11 |
| CHEMBL8260 | BAICALEIN | 2.0 | 1 | 4.00 |
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | - |
| CHEMBL289277 | EMODIN | — | 1 | - |
| CHEMBL210635 | GENKWANIN | — | 1 | - |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | - |
| CHEMBL117 | CHRYSIN | — | 1 | - |
| CHEMBL242385 | — | — | 1 | - |
| CHEMBL455581 | — | — | 1 | - |
| CHEMBL53418 | DANTHRON | 4.0 | 1 | - |
| CHEMBL484662 | — | — | 1 | - |
| CHEMBL294878 | — | — | 1 | - |
| CHEMBL200715 | (-)-CATECHIN | — | 1 | - |
| CHEMBL16807 | 5-HYDROXYFLAVONE | — | 1 | - |
| CHEMBL243664 | ACACETIN | — | 1 | - |
| CHEMBL448297 | SAKURANETIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1089732 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL418068 | RHEIN | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL164 | MYRICETIN | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL247484 | TRICETIN | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL55415 | SCUTELLAREIN | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL50 | QUERCETIN | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL28 | APIGENIN | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL8260 | BAICALEIN | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL150 | KAEMPFEROL | IC50 | = | 110000.0 | nM | - |
| CHEMBL289277 | EMODIN | IC50 | = | 110000.0 | nM | - |
| CHEMBL210635 | GENKWANIN | IC50 | = | 140000.0 | nM | - |
| CHEMBL44 | GENISTEIN | IC50 | = | 230000.0 | nM | - |
| CHEMBL117 | CHRYSIN | IC50 | = | 340000.0 | nM | - |
| CHEMBL242385 | — | IC50 | = | 360000.0 | nM | - |
| CHEMBL455581 | — | IC50 | = | 430000.0 | nM | - |
| CHEMBL53418 | DANTHRON | IC50 | = | 710000.0 | nM | - |
| CHEMBL484662 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL294878 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL200715 | (-)-CATECHIN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL16807 | 5-HYDROXYFLAVONE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL243664 | ACACETIN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL448297 | SAKURANETIN | IC50 | > | 1000000.0 | nM | - |