Assay Detail
Binding
CHEMBL947847
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Inhibition of human intestinal CE-mediated O-nitrophenyl acetate hydrolysis by spectrophotometry
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Improved, selective, human intestinal carboxylesterase inhibitors designed to modulate 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (Irinotecan; CPT-11) toxicity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 57 | 6.56 | 7.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486072 | — | — | 1 | 7.86 |
| CHEMBL491262 | — | — | 1 | 7.73 |
| CHEMBL487300 | — | — | 1 | 7.67 |
| CHEMBL489006 | — | — | 1 | 7.63 |
| CHEMBL486277 | — | — | 1 | 7.63 |
| CHEMBL483471 | — | — | 1 | 7.38 |
| CHEMBL254426 | — | — | 1 | 7.27 |
| CHEMBL482847 | — | — | 1 | 7.17 |
| CHEMBL482640 | — | — | 1 | 7.13 |
| CHEMBL482848 | — | — | 1 | 7.07 |
| CHEMBL487299 | — | — | 1 | 7.04 |
| CHEMBL482441 | — | — | 1 | 7.04 |
| CHEMBL519501 | — | — | 1 | 6.92 |
| CHEMBL521499 | — | — | 1 | 6.80 |
| CHEMBL482650 | — | — | 1 | 6.79 |
| CHEMBL451609 | — | — | 1 | 6.78 |
| CHEMBL484276 | — | — | 1 | 6.71 |
| CHEMBL483071 | — | — | 1 | 6.71 |
| CHEMBL485244 | — | — | 1 | 6.70 |
| CHEMBL485107 | — | — | 1 | 6.68 |
| CHEMBL488335 | — | — | 1 | 6.66 |
| CHEMBL519326 | — | — | 1 | 6.62 |
| CHEMBL485106 | — | — | 1 | 6.61 |
| CHEMBL483676 | — | — | 1 | 6.61 |
| CHEMBL483683 | — | — | 1 | 6.57 |
| CHEMBL483072 | — | — | 1 | 6.56 |
| CHEMBL482853 | — | — | 1 | 6.55 |
| CHEMBL489005 | — | — | 1 | 6.50 |
| CHEMBL492066 | — | — | 1 | 6.46 |
| CHEMBL482639 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486072 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL491262 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL487300 | — | Ki | = | 21.2 | nM | 7.67 |
| CHEMBL489006 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL486277 | — | Ki | = | 23.5 | nM | 7.63 |
| CHEMBL483471 | — | Ki | = | 41.5 | nM | 7.38 |
| CHEMBL254426 | — | Ki | = | 53.2 | nM | 7.27 |
| CHEMBL482847 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL482640 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL482848 | — | Ki | = | 85.2 | nM | 7.07 |
| CHEMBL487299 | — | Ki | = | 90.8 | nM | 7.04 |
| CHEMBL482441 | — | Ki | = | 91.5 | nM | 7.04 |
| CHEMBL519501 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL521499 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL482650 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL451609 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL484276 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL483071 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL485244 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL485107 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL488335 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL519326 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL485106 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL483676 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL483683 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL483072 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL482853 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL489005 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL492066 | — | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL482639 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL509333 | — | Ki | = | 365.0 | nM | 6.44 |
| CHEMBL521447 | — | Ki | = | 385.0 | nM | 6.42 |
| CHEMBL1162998 | — | Ki | = | 385.0 | nM | 6.42 |
| CHEMBL483470 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL487102 | — | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL482854 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL485245 | — | Ki | = | 488.0 | nM | 6.31 |
| CHEMBL521292 | — | Ki | = | 568.0 | nM | 6.25 |
| CHEMBL488111 | — | Ki | = | 693.0 | nM | 6.16 |
| CHEMBL448073 | — | Ki | = | 696.0 | nM | 6.16 |
| CHEMBL454233 | — | Ki | = | 767.0 | nM | 6.12 |
| CHEMBL484275 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL499975 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL483675 | — | Ki | = | 1450.0 | nM | 5.84 |
| CHEMBL483467 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL491256 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL521464 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL489652 | — | Ki | = | 2060.0 | nM | 5.69 |
| CHEMBL492067 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL483468 | — | Ki | = | 3240.0 | nM | 5.49 |