Assay Detail
ADMET
CHEMBL2396489
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Inhibition of CYP2C9 in human liver microsomes after 30 mins
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.30 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2391572 | — | — | 1 | 7.17 |
| CHEMBL2393185 | — | — | 1 | 7.13 |
| CHEMBL2393168 | — | — | 1 | 6.96 |
| CHEMBL2393176 | — | — | 1 | 6.90 |
| CHEMBL2391551 | — | — | 1 | 6.86 |
| CHEMBL2393188 | — | — | 1 | 6.83 |
| CHEMBL2391567 | — | — | 1 | 6.70 |
| CHEMBL2393187 | — | — | 1 | 6.34 |
| CHEMBL2393186 | — | — | 1 | 6.29 |
| CHEMBL2393159 | — | — | 1 | 6.26 |
| CHEMBL2393191 | — | — | 1 | 6.22 |
| CHEMBL2393177 | — | — | 1 | 6.19 |
| CHEMBL2393190 | — | — | 1 | 6.12 |
| CHEMBL2393167 | — | — | 1 | 6.03 |
| CHEMBL2393158 | — | — | 1 | 5.98 |
| CHEMBL2393160 | — | — | 1 | 5.94 |
| CHEMBL2393180 | — | — | 1 | 5.89 |
| CHEMBL2393182 | — | — | 1 | 5.75 |
| CHEMBL2393178 | — | — | 1 | 5.71 |
| CHEMBL2393166 | — | — | 1 | 5.66 |
| CHEMBL2393192 | — | — | 1 | 5.34 |
| CHEMBL2393174 | — | — | 1 | - |
| CHEMBL2393175 | — | — | 1 | - |
| CHEMBL2393171 | — | — | 1 | - |
| CHEMBL2393193 | — | — | 1 | - |
| CHEMBL2393179 | — | — | 1 | - |
| CHEMBL2393170 | — | — | 1 | - |
| CHEMBL2393172 | — | — | 1 | - |
| CHEMBL2393181 | — | — | 1 | - |
| CHEMBL2393183 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2391572 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2393185 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2393168 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2393176 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL2391551 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL2393188 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL2391567 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2393187 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2393186 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL2393159 | — | IC50 | = | 554.0 | nM | 6.26 |
| CHEMBL2393191 | — | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL2393177 | — | IC50 | = | 644.0 | nM | 6.19 |
| CHEMBL2393190 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2393167 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL2393158 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL2393160 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL2393180 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2393182 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL2393178 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL2393166 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL2393192 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL2393183 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393165 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393164 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393163 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393162 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393161 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393189 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393173 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393184 | — | IC50 | - | — | - | |
| CHEMBL2393181 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393172 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393179 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393193 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393171 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393175 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2393174 | — | IC50 | > | 10000.0 | nM | - |