Assay Detail
Binding
CHEMBL5225647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human recombinant ME3 (26 to 604 residues) using L-malate and beta-NADP+ as substrate preincubated with enzyme for 5 mins followed by beta-NADP+ challenge and incubated under shaking for 5 mins followed by incubation for 3 hrs without shaking by resorufin dye based fluorescence analysis
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
NADP-dependent malic enzyme, mitochondrial (CHEMBL6182) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
In the Quest for Potent and Selective Malic Enzyme 3 Inhibitors for the Treatment of Pancreatic Ductal Adenocarcinoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.58 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5284610 | — | — | 1 | 7.22 |
| CHEMBL5285899 | — | — | 1 | 7.16 |
| CHEMBL5275653 | — | — | 1 | 7.10 |
| CHEMBL5287773 | — | — | 1 | 7.05 |
| CHEMBL5284469 | — | — | 1 | 7.00 |
| CHEMBL5289840 | — | — | 1 | 7.00 |
| CHEMBL5289950 | — | — | 1 | 6.96 |
| CHEMBL5278951 | — | — | 1 | 6.96 |
| CHEMBL5277536 | — | — | 1 | 6.92 |
| CHEMBL5288731 | — | — | 1 | 6.89 |
| CHEMBL5279230 | — | — | 1 | 6.89 |
| CHEMBL5279096 | — | — | 1 | 6.89 |
| CHEMBL5273550 | — | — | 1 | 6.85 |
| CHEMBL372408 | — | — | 1 | 6.82 |
| CHEMBL5267542 | — | — | 1 | 6.82 |
| CHEMBL5279589 | — | — | 1 | 6.80 |
| CHEMBL5278596 | — | — | 1 | 6.70 |
| CHEMBL5281297 | — | — | 1 | 6.64 |
| CHEMBL5286488 | — | — | 1 | 6.62 |
| CHEMBL5290463 | — | — | 1 | 6.60 |
| CHEMBL5274945 | — | — | 1 | 6.51 |
| CHEMBL5283020 | — | — | 1 | 6.48 |
| CHEMBL5286064 | — | — | 1 | 6.44 |
| CHEMBL5291081 | — | — | 1 | 6.41 |
| CHEMBL5282439 | — | — | 1 | 6.39 |
| CHEMBL5270965 | — | — | 1 | 6.33 |
| CHEMBL5281258 | — | — | 1 | 6.24 |
| CHEMBL5218866 | — | — | 1 | 6.05 |
| CHEMBL5283717 | — | — | 1 | 5.29 |
| CHEMBL5277143 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5284610 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5285899 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5275653 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5287773 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5284469 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5289840 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5289950 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5278951 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5277536 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5288731 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5279230 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5279096 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5273550 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL372408 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5267542 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5279589 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5278596 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5281297 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5286488 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5290463 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5274945 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5283020 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5286064 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5291081 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5282439 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5270965 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5281258 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5218866 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5283717 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5277143 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL5267207 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL5268726 | — | IC50 | - | — | - | |
| CHEMBL5284509 | — | IC50 | - | — | - | |
| CHEMBL5274665 | — | IC50 | - | — | - |