Assay Detail
Binding
CHEMBL2174120
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Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 2 hrs by resazurin/diaphorasecoupled assay
48
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glucose-6-phosphate 1-dehydrogenase (CHEMBL2169726) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 5.04 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170943 | — | — | 1 | 6.05 |
| CHEMBL2170936 | — | — | 1 | 5.85 |
| CHEMBL2170938 | — | — | 1 | 5.78 |
| CHEMBL2171113 | — | — | 1 | 5.76 |
| CHEMBL2170935 | — | — | 1 | 5.63 |
| CHEMBL2170940 | — | — | 1 | 5.62 |
| CHEMBL2170929 | — | — | 1 | 5.59 |
| CHEMBL2170945 | — | — | 1 | 5.51 |
| CHEMBL2170939 | — | — | 1 | 5.37 |
| CHEMBL2170930 | — | — | 1 | 5.36 |
| CHEMBL2170937 | — | — | 1 | 5.24 |
| CHEMBL2171111 | — | — | 1 | 5.23 |
| CHEMBL2170933 | — | — | 1 | 5.23 |
| CHEMBL2170944 | — | — | 1 | 5.18 |
| CHEMBL2170923 | — | — | 2 | 5.16 |
| CHEMBL2170932 | — | — | 1 | 5.08 |
| CHEMBL2170922 | — | — | 1 | 5.06 |
| CHEMBL1337166 | — | — | 1 | 5.03 |
| CHEMBL2170912 | — | — | 2 | 5.02 |
| CHEMBL2170934 | — | — | 1 | 5.01 |
| CHEMBL2170914 | — | — | 1 | 4.96 |
| CHEMBL2170915 | — | — | 1 | 4.93 |
| CHEMBL2170925 | — | — | 1 | 4.84 |
| CHEMBL2170924 | — | — | 1 | 4.79 |
| CHEMBL2171112 | — | — | 2 | 4.78 |
| CHEMBL2170931 | — | — | 1 | 4.75 |
| CHEMBL2170916 | — | — | 1 | 4.67 |
| CHEMBL2170909 | — | — | 1 | 4.64 |
| CHEMBL2170919 | — | — | 1 | 4.39 |
| CHEMBL2170910 | — | — | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170943 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2170936 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL2170938 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL2171113 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL2170935 | — | IC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL2170940 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL2170929 | — | IC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL2170945 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2170939 | — | IC50 | = | 4280.0 | nM | 5.37 |
| CHEMBL2170930 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL2170937 | — | IC50 | = | 5720.0 | nM | 5.24 |
| CHEMBL2171111 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2170933 | — | IC50 | = | 5930.0 | nM | 5.23 |
| CHEMBL2170944 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2170923 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2170923 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2170932 | — | IC50 | = | 8230.0 | nM | 5.08 |
| CHEMBL2170922 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL1337166 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL2170912 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL2170934 | — | IC50 | = | 9790.0 | nM | 5.01 |
| CHEMBL2170914 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL2170915 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL2170925 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL2170924 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL2170912 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL2171112 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL2171112 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL2170931 | — | IC50 | = | 17900.0 | nM | 4.75 |
| CHEMBL2170916 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL2170909 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL2170919 | — | IC50 | = | 40900.0 | nM | 4.39 |
| CHEMBL2170910 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL2170918 | — | IC50 | = | 46600.0 | nM | 4.33 |
| CHEMBL2170913 | — | IC50 | = | 49700.0 | nM | 4.30 |
| CHEMBL2170926 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL2170920 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL2170941 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170942 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2171110 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2169897 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170921 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170927 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170928 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170917 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170907 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170908 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL2170911 | — | IC50 | > | 80000.0 | nM | - |