Assay Detail
Binding
CHEMBL5731079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Human P-LAP (hP-LAP) Assay: HEK293 cells forced to transiently express hP-LAP (J Biol Chem 1996; 271: 56-61) were prepared by lipofection, homogenized, and then subjected to ultracentrifugation at 100,000×g for 30 minutes. Microsomes containing hP-LAP were thereby prepared. The microsomes (with a total protein content of 0.5 to 1.5 μg/well) were mixed with a solvent (DMSO; final concentration: 0.1%) or with each test compound (common ratio: 3; maximum concentration: 10 μM). AVP was then added to the solution into a final concentration of 25 μM, and the resulting solution was allowed to react for one hour at 37° C. An aqueous 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 logistic regression to evaluate inhibition of human P-LAP (hP-LAP) activity. The results are shown in Tables 1 and 2 and indicate that the example compounds effectively inhibit AVP degradation by hP-LAP.
420
Total Activities
140
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyridine derivative
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 140 | 8.13 | 9.05 |
| kon | 140 | - | - |
| k_off | 140 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5858644 | — | — | 3 | 9.05 |
| CHEMBL6013513 | — | — | 3 | 9.03 |
| CHEMBL6020816 | — | — | 3 | 9.02 |
| CHEMBL5847848 | — | — | 3 | 9.00 |
| CHEMBL5900568 | — | — | 3 | 8.92 |
| CHEMBL5845804 | — | — | 3 | 8.89 |
| CHEMBL6046862 | — | — | 3 | 8.89 |
| CHEMBL5925746 | — | — | 3 | 8.89 |
| CHEMBL5832194 | — | — | 3 | 8.85 |
| CHEMBL5983220 | — | — | 3 | 8.82 |
| CHEMBL5875249 | — | — | 3 | 8.82 |
| CHEMBL5889833 | — | — | 3 | 8.82 |
| CHEMBL5744859 | — | — | 3 | 8.80 |
| CHEMBL5966636 | — | — | 3 | 8.80 |
| CHEMBL5897593 | — | — | 3 | 8.80 |
| CHEMBL5825133 | — | — | 3 | 8.74 |
| CHEMBL5924278 | — | — | 3 | 8.74 |
| CHEMBL6001237 | — | — | 3 | 8.74 |
| CHEMBL6053091 | — | — | 3 | 8.74 |
| CHEMBL5765662 | — | — | 3 | 8.72 |
| CHEMBL5767114 | — | — | 3 | 8.72 |
| CHEMBL5848269 | — | — | 3 | 8.70 |
| CHEMBL5837864 | — | — | 3 | 8.68 |
| CHEMBL5850219 | — | — | 3 | 8.64 |
| CHEMBL5901071 | — | — | 3 | 8.64 |
| CHEMBL5848118 | — | — | 3 | 8.62 |
| CHEMBL5996078 | — | — | 3 | 8.60 |
| CHEMBL5813338 | — | — | 3 | 8.59 |
| CHEMBL5801079 | — | — | 3 | 8.59 |
| CHEMBL5756198 | — | — | 3 | 8.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5858644 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL6013513 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL6020816 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5847848 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5900568 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL6046862 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5925746 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5845804 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5832194 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5889833 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5875249 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5983220 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5744859 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5966636 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5897593 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL6053091 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5924278 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6001237 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5825133 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5765662 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5767114 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5848269 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5837864 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5850219 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5901071 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5848118 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5996078 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5813338 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5801079 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5756198 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5929981 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5841906 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5986707 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5757179 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5979812 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5950078 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5979564 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5833643 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5952906 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5916674 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL6055514 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL6037274 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5995260 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5999116 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5877142 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5760266 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6006000 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5829765 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5855958 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5873538 | — | IC50 | = | 4.1 | nM | 8.39 |