Assay Detail
Binding
CHEMBL801253
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required for 50% in vitro inhibition of recombinant human sorbitol dehydrogenase (h-SDH)
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Orally-effective, long-acting sorbitol dehydrogenase inhibitors: synthesis, structure-activity relationships, and in vivo evaluations of novel heterocycle-substituted piperazino-pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.17 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL151486 | — | — | 1 | 8.10 |
| CHEMBL151017 | — | — | 1 | 8.00 |
| CHEMBL147064 | — | — | 1 | 7.92 |
| CHEMBL347716 | — | — | 1 | 7.92 |
| CHEMBL151615 | — | — | 1 | 7.70 |
| CHEMBL151439 | — | — | 1 | 7.64 |
| CHEMBL149048 | — | — | 1 | 7.64 |
| CHEMBL348496 | — | — | 1 | 7.62 |
| CHEMBL359089 | — | — | 1 | 7.51 |
| CHEMBL151311 | — | — | 1 | 7.50 |
| CHEMBL346418 | — | — | 1 | 7.47 |
| CHEMBL150642 | — | — | 1 | 7.46 |
| CHEMBL359168 | — | — | 1 | 7.44 |
| CHEMBL151764 | — | — | 1 | 7.43 |
| CHEMBL149981 | — | — | 1 | 7.40 |
| CHEMBL556517 | — | — | 1 | 7.36 |
| CHEMBL150296 | — | — | 1 | 7.23 |
| CHEMBL146805 | — | — | 1 | 7.19 |
| CHEMBL151394 | — | — | 1 | 7.17 |
| CHEMBL150734 | — | — | 1 | 7.14 |
| CHEMBL356692 | — | — | 1 | 7.10 |
| CHEMBL348427 | — | — | 1 | 7.10 |
| CHEMBL150803 | — | — | 1 | 7.10 |
| CHEMBL151605 | — | — | 1 | 7.06 |
| CHEMBL151268 | — | — | 1 | 7.03 |
| CHEMBL151560 | — | — | 1 | 7.00 |
| CHEMBL149409 | — | — | 1 | 7.00 |
| CHEMBL347575 | — | — | 1 | 6.96 |
| CHEMBL357712 | — | — | 1 | 6.92 |
| CHEMBL151690 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL151486 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL151017 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL347716 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL147064 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL151615 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL151439 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL149048 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL348496 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL359089 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL151311 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL346418 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL150642 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL359168 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL151764 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL149981 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL556517 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL150296 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL146805 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL151394 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL150734 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL150803 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL356692 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL348427 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL151605 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL151268 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL151560 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL149409 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL347575 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL357712 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL151690 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL346682 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL148936 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL423753 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL358327 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL151567 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL147197 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL345259 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL148436 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL148647 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL151602 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL151704 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL90488 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL348663 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL345725 | — | IC50 | = | 270.0 | nM | 6.57 |