Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
molecular modeling using PDB-structures 2B8L and 3FKT, with inhibitor 6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole | inhibitor of BACE1, EC 3.4.23.46. 150fold more effective on BACE1 than BACE2 | Homo sapiens | |
6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole | inhibitor of BACE1, EC 3.4.23.46. 200fold more effective on BACE1 than BACE2 | Homo sapiens | |
6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole | inhibitor of BACE1, EC 3.4.23.46. 100fold more effective on BACE1 than BACE2 | Homo sapiens |
Organic Solvent | Comment | Organism |
---|---|---|
dimethyl sulfoxide | assay in 3.3% final concentration | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P56817 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
rhodamine-EVNLDAEFK-quencher + H2O | FRET-substrate | Homo sapiens | ? | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000017 | - |
6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole | pH 4.5, 25°C | Homo sapiens | |
0.000025 | - |
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole | pH 4.5, 25°C | Homo sapiens | |
0.000034 | - |
6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole | pH 4.5, 25°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000026 | - |
pH 4.5, 25°C | Homo sapiens | 2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole | |
0.000035 | - |
pH 4.5, 25°C | Homo sapiens | 6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole | |
0.0018 | - |
pH 4.5, 25°C | Homo sapiens | 6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole |