Assay Detail
Binding
CHEMBL5736672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Activity Assay: IRAP: Rat epididymal fat pads were homogenized and subjected to ultracentrifugation at 100,000×g for 30 minutes to obtain microsomes containing IRAP. The microsomes (with a total protein content of 55 μg/well) were mixed with a solvent (dimethyl sulfoxide; hereinafter, abbreviated as DMSO (final concentration: 0.1%)) or with each test compound (common ratio: 3; maximum concentration: 10 μM). AVP was then added to the solution to a final concentration of 25 μM, and the resulting solution was allowed to react for one hour at 37° C. An aqueous trifluoroacetic acid (hereinafter, abbreviated as TFA) solution was then added to the solution (final concentration: 1%) to stop the enzymatic reaction. Residual AVP was then determined by mass spectrometry (MALDI-MS). Based on the results, IC50 values (nM), i.e. concentrations required for 50% inhibition of decrease in AVP level in the solvent control group, of the individual test compounds were calculated by the logistic regression to evaluate inhibition of IRAP activity
450
Total Activities
150
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyridine derivative
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 150 | 8.21 | 9.38 |
| kon | 150 | - | - |
| k_off | 150 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5858644 | — | — | 3 | 9.38 |
| CHEMBL5767114 | — | — | 3 | 9.21 |
| CHEMBL6013513 | — | — | 3 | 9.11 |
| CHEMBL5925746 | — | — | 3 | 9.11 |
| CHEMBL5953760 | — | — | 3 | 9.05 |
| CHEMBL5757179 | — | — | 3 | 9.04 |
| CHEMBL6006468 | — | — | 3 | 9.04 |
| CHEMBL6020816 | — | — | 3 | 9.00 |
| CHEMBL5832194 | — | — | 3 | 9.00 |
| CHEMBL5823653 | — | — | 3 | 9.00 |
| CHEMBL5897593 | — | — | 3 | 8.96 |
| CHEMBL5900568 | — | — | 3 | 8.96 |
| CHEMBL5845804 | — | — | 3 | 8.92 |
| CHEMBL5841906 | — | — | 3 | 8.92 |
| CHEMBL5901071 | — | — | 3 | 8.92 |
| CHEMBL5847848 | — | — | 3 | 8.89 |
| CHEMBL5950078 | — | — | 3 | 8.89 |
| CHEMBL6046862 | — | — | 3 | 8.85 |
| CHEMBL5916674 | — | — | 3 | 8.82 |
| CHEMBL5952906 | — | — | 3 | 8.82 |
| CHEMBL5889833 | — | — | 3 | 8.82 |
| CHEMBL5796475 | — | — | 3 | 8.82 |
| CHEMBL5996078 | — | — | 3 | 8.80 |
| CHEMBL5910023 | — | — | 3 | 8.80 |
| CHEMBL5848118 | — | — | 3 | 8.77 |
| CHEMBL5790439 | — | — | 3 | 8.77 |
| CHEMBL5815194 | — | — | 3 | 8.77 |
| CHEMBL5801596 | — | — | 3 | 8.77 |
| CHEMBL5995214 | — | — | 3 | 8.74 |
| CHEMBL6041378 | — | — | 3 | 8.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5858644 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5767114 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5925746 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL6013513 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL5953760 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5757179 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL6006468 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL6020816 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5832194 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5823653 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5900568 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5897593 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5841906 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5845804 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5901071 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5950078 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5847848 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL6046862 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5916674 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5889833 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5796475 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5952906 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5996078 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5910023 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5790439 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5801596 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5848118 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5815194 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5995214 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5848269 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6041378 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6043945 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5929981 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5930294 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5837864 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6001237 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5850219 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5924278 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6037274 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6053091 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5979564 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5813598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5966636 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5875249 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5901450 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5955336 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5873538 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5969842 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5952961 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5894576 | — | IC50 | = | 2.4 | nM | 8.62 |