Assay Detail
Binding
CHEMBL3705358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Experimental was performed by measuring the formation of NADH at 340 nm with a fluorescence spectrophotometer. Specifically, 2 ml (in total) of the solution containing 50 mM Tris-HCl (pH 7.5), 0.1 mM DTT, 0.25 mM NAD+, 10 μg of purified 15-PGDH enzyme, 21 μM PGE2 and various concentrations (0.0001 μM to 64 μM) of the derivatives according to the present invention was added to each cell. The absorbance of the reaction mixture was recorded at 340 nm so that the activities of the derivatives according to the present invention as 15-PGDH inhibitors were determined from a standard curve prepared from the absorbance of various concentrations of NADH at 340 nm.
130
Total Activities
124
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
15-hydroxyprostaglandin dehydrogenase [NAD(+)] (CHEMBL1293255) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thiazolidinedione derivative and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 130 | 6.50 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800140 | — | — | 1 | 8.18 |
| CHEMBL1800139 | — | — | 1 | 8.14 |
| CHEMBL1800143 | — | — | 1 | 7.99 |
| CHEMBL4114817 | — | — | 1 | 7.75 |
| CHEMBL2414240 | — | — | 1 | 7.71 |
| CHEMBL2414160 | — | — | 1 | 7.70 |
| CHEMBL4114745 | — | — | 1 | 7.69 |
| CHEMBL4114682 | — | — | 1 | 7.66 |
| CHEMBL4114752 | — | — | 1 | 7.64 |
| CHEMBL1800144 | — | — | 1 | 7.58 |
| CHEMBL1800142 | — | — | 1 | 7.57 |
| CHEMBL4115685 | — | — | 1 | 7.55 |
| CHEMBL4114683 | — | — | 1 | 7.50 |
| CHEMBL2414161 | — | — | 1 | 7.42 |
| CHEMBL84603 | — | — | 1 | 7.37 |
| CHEMBL4114746 | — | — | 1 | 7.35 |
| CHEMBL2414159 | — | — | 1 | 7.32 |
| CHEMBL2414162 | — | — | 1 | 7.32 |
| CHEMBL1800141 | — | — | 1 | 7.31 |
| CHEMBL4114657 | — | — | 1 | 7.30 |
| CHEMBL4114816 | — | — | 1 | 7.30 |
| CHEMBL3685339 | — | — | 1 | 7.29 |
| CHEMBL599406 | — | — | 1 | 7.29 |
| CHEMBL2414165 | — | — | 1 | 7.28 |
| CHEMBL4114728 | — | — | 1 | 7.26 |
| CHEMBL4114781 | — | — | 1 | 7.26 |
| CHEMBL4115691 | — | — | 1 | 7.24 |
| CHEMBL4114756 | — | — | 1 | 7.23 |
| CHEMBL3685346 | — | — | 1 | 7.22 |
| CHEMBL3685344 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800140 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL1800139 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL1800143 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4114817 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL2414240 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL2414160 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4114745 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL4114682 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL4114752 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1800144 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL1800142 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL4115685 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL4114683 | — | IC50 | = | 31.4 | nM | 7.50 |
| CHEMBL2414161 | — | IC50 | = | 38.1 | nM | 7.42 |
| CHEMBL84603 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL4114746 | — | IC50 | = | 44.9 | nM | 7.35 |
| CHEMBL2414162 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL2414159 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL1800141 | — | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL4114816 | — | IC50 | = | 50.6 | nM | 7.30 |
| CHEMBL4114657 | — | IC50 | = | 49.8 | nM | 7.30 |
| CHEMBL3685339 | — | IC50 | = | 50.8 | nM | 7.29 |
| CHEMBL599406 | — | IC50 | = | 50.9 | nM | 7.29 |
| CHEMBL2414165 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4114781 | — | IC50 | = | 54.3 | nM | 7.26 |
| CHEMBL4114728 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4115691 | — | IC50 | = | 57.6 | nM | 7.24 |
| CHEMBL4114756 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3685346 | — | IC50 | = | 59.5 | nM | 7.22 |
| CHEMBL3685344 | — | IC50 | = | 62.2 | nM | 7.21 |
| CHEMBL599018 | — | IC50 | = | 66.4 | nM | 7.18 |
| CHEMBL3685338 | — | IC50 | = | 71.9 | nM | 7.14 |
| CHEMBL2414166 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2414140 | — | IC50 | = | 84.1 | nM | 7.08 |
| CHEMBL4114768 | — | IC50 | = | 94.5 | nM | 7.03 |
| CHEMBL4115690 | — | IC50 | = | 94.5 | nM | 7.03 |
| CHEMBL590265 | — | IC50 | = | 95.9 | nM | 7.02 |
| CHEMBL2414145 | — | IC50 | = | 99.3 | nM | 7.00 |
| CHEMBL4114786 | — | IC50 | = | 104.3 | nM | 6.98 |
| CHEMBL3685368 | — | IC50 | = | 109.8 | nM | 6.96 |
| CHEMBL598397 | — | IC50 | = | 114.6 | nM | 6.94 |
| CHEMBL3685350 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4115688 | — | IC50 | = | 122.2 | nM | 6.91 |
| CHEMBL591466 | — | IC50 | = | 124.5 | nM | 6.91 |
| CHEMBL3685395 | — | IC50 | = | 125.1 | nM | 6.90 |
| CHEMBL3685369 | — | IC50 | = | 136.5 | nM | 6.87 |
| CHEMBL3685375 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3685400 | — | IC50 | = | 142.8 | nM | 6.84 |
| CHEMBL610221 | — | IC50 | = | 148.5 | nM | 6.83 |
| CHEMBL4114747 | — | IC50 | = | 153.9 | nM | 6.81 |