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Literature summary for 3.4.22.15 extracted from
- Screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity (2016), Chem. Biol. Drug Des., 87, 154-158 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression of rhodesain in Pichia pastoris | Trypanosoma brucei rhodesiense |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide) | - |
Homo sapiens |  |
| (N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide) | - |
Trypanosoma brucei brucei | |
| (N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide) | - |
Trypanosoma brucei rhodesiense | |
| 2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol | - |
Homo sapiens | |
| 2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol | - |
Trypanosoma brucei brucei | |
| 2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol | the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM | Trypanosoma brucei rhodesiense | |
| 2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | - |
Homo sapiens | |
| 2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | - |
Trypanosoma brucei brucei | |
| 2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | - |
Trypanosoma brucei rhodesiense | |
| 2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Homo sapiens | |
| 2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Trypanosoma brucei rhodesiense | |
| 2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Homo sapiens | |
| 2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Trypanosoma brucei rhodesiense | |
| 2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | - |
Homo sapiens | |
| 2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | - |
Trypanosoma brucei rhodesiense | |
| 2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Homo sapiens | |
| 2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | - |
Trypanosoma brucei rhodesiense | |
| 2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide | - |
Homo sapiens | |
| 2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide | - |
Trypanosoma brucei brucei | |
| 2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide | - |
Trypanosoma brucei rhodesiense | |
| 2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | - |
Homo sapiens | |
| 2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | - |
Trypanosoma brucei rhodesiense | |
| 4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline | - |
Homo sapiens | |
| 4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline | - |
Trypanosoma brucei brucei | |
| 4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline | has H-bond and steric interactions with Cys 25 of rhodesain's catalytic triad as well as residues Leu67 and Met68 while its dianiline motifs have steric interactions with Gly64 and Leu160 | Trypanosoma brucei rhodesiense | |
| 4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid | - |
Homo sapiens | |
| 4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid | - |
Trypanosoma brucei brucei | |
| 4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid | - |
Trypanosoma brucei rhodesiense | |
| 4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol | - |
Homo sapiens | |
| 4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol | - |
Trypanosoma brucei brucei | |
| 4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol | - |
Trypanosoma brucei rhodesiense | |
| 4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide | - |
Homo sapiens | |
| 4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide | - |
Trypanosoma brucei brucei | |
| 4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide | the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM | Trypanosoma brucei rhodesiense | |
| 4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide | - |
Homo sapiens | |
| 4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide | - |
Trypanosoma brucei brucei | |
| 4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide | the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM | Trypanosoma brucei rhodesiense | |
| 4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol | - |
Homo sapiens | |
| 4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol | - |
Trypanosoma brucei brucei | |
| 4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol | - |
Trypanosoma brucei rhodesiense | |
| 4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline | - |
Homo sapiens | |
| 4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline | - |
Trypanosoma brucei brucei | |
| 4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline | - |
Trypanosoma brucei rhodesiense | |
| 4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | - |
Homo sapiens | |
| 4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | - |
Trypanosoma brucei brucei | |
| 4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | - |
Trypanosoma brucei rhodesiense | |
| 4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole) | - |
Homo sapiens | |
| 4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole) | - |
Trypanosoma brucei brucei | |
| 4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole) | - |
Trypanosoma brucei rhodesiense | |
| 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole | - |
Homo sapiens | |
| 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole | the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM | Trypanosoma brucei rhodesiense | |
| 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole | - |
Homo sapiens | |
| 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole | - |
Trypanosoma brucei brucei | |
| 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole | - |
Trypanosoma brucei rhodesiense | |
| bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone | - |
Homo sapiens | |
| bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone | - |
Trypanosoma brucei brucei | |
| bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone | the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM | Trypanosoma brucei rhodesiense | |
| additional information | screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview | Homo sapiens | |
| additional information | screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview | Trypanosoma brucei brucei | |
| additional information | screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview. No inhibition by 7 and 13 | Trypanosoma brucei rhodesiense | |
| N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide | - |
Homo sapiens | |
| N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide | - |
Trypanosoma brucei brucei | |
| N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide | the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM | Trypanosoma brucei rhodesiense | |
| N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide | - |
Homo sapiens | |
| N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide | - |
Trypanosoma brucei brucei | |
| N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide | - |
Trypanosoma brucei rhodesiense | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P07711 | - |
- |
| Trypanosoma brucei brucei | Q95PM0 | - |
- |
| Trypanosoma brucei brucei 427 | Q95PM0 | - |
- |
| Trypanosoma brucei rhodesiense | Q95PM0 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant rhodesain from Pichia pastoris | Trypanosoma brucei rhodesiense |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| Hep-G2 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O | - |
Trypanosoma brucei rhodesiense | benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin | - |
? | |
| benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O | - |
Trypanosoma brucei brucei | benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin | - |
? | |
| benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O | - |
Trypanosoma brucei brucei 427 | benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| cathepsin L-like protein | - |
Homo sapiens |
| cathepsin L-like protein | - |
Trypanosoma brucei rhodesiense |
| cathepsin L-like protein | - |
Trypanosoma brucei brucei |
| rhodesain | - |
Trypanosoma brucei rhodesiense |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | - |
assay at | Trypanosoma brucei rhodesiense |
| 37 | - |
in vivo assay at | Homo sapiens |
| 37 | - |
in vivo assay at | Trypanosoma brucei brucei |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 5.5 | - |
assay at | Trypanosoma brucei rhodesiense |
| 7.4 | - |
in vivo assay at | Homo sapiens |
| 7.4 | - |
in vivo assay at | Trypanosoma brucei brucei |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00047 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline | |
| 0.00056 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol | |
| 0.00089 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline | |
| 0.0011 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone | |
| 0.00178 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide | |
| 0.00193 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline | |
| 0.00215 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide | |
| 0.00236 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol | |
| 0.00241 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.00283 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide | |
| 0.00304 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide | |
| 0.00338 | - |
pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole | |
| 0.0058 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline | |
| 0.00981 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol | |
| 0.01179 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol | |
| 0.01293 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.01475 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.01706 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole | |
| 0.01749 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | |
| 0.01831 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole | |
| 0.01932 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | 4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole) | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone | |
| 0.02 | - |
above, pH 7.4, 37°C | Trypanosoma brucei brucei | N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole) | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole | |
| 0.02 | - |
above, pH 5.5, 25°C | Trypanosoma brucei rhodesiense | N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide | |
| 0.02002 | - |
pH 7.4, 37°C | Trypanosoma brucei brucei | 2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.0402 | - |
pH 7.4, 37°C | Homo sapiens | 2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | |
| 0.0621 | - |
pH 7.4, 37°C | Homo sapiens | 4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol | |
| 0.0625 | - |
pH 7.4, 37°C | Homo sapiens | N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide | |
| 0.0655 | - |
pH 7.4, 37°C | Homo sapiens | 4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole) | |
| 0.074 | - |
pH 7.4, 37°C | Homo sapiens | 2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole | |
| 0.0808 | - |
pH 7.4, 37°C | Homo sapiens | 2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.0818 | - |
pH 7.4, 37°C | Homo sapiens | 2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.0834 | - |
pH 7.4, 37°C | Homo sapiens | 4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide | |
| 0.0847 | - |
pH 7.4, 37°C | Homo sapiens | 4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline | |
| 0.0862 | - |
pH 7.4, 37°C | Homo sapiens | N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide | |
| 0.0863 | - |
pH 7.4, 37°C | Homo sapiens | 2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole | |
| 0.0865 | - |
pH 7.4, 37°C | Homo sapiens | 4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid | |
| 0.087 | - |
pH 7.4, 37°C | Homo sapiens | 2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | |
| 0.08835 | - |
pH 7.4, 37°C | Homo sapiens | 4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol | |
| 0.0888 | - |
pH 7.4, 37°C | Homo sapiens | 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole | |
| 0.0922 | - |
pH 7.4, 37°C | Homo sapiens | 4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide | |
| 0.0927 | - |
pH 7.4, 37°C | Homo sapiens | 2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide | |
| 0.0972 | - |
pH 7.4, 37°C | Homo sapiens | bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone | |
| 0.0981 | - |
pH 7.4, 37°C | Homo sapiens | 5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole | |
| 0.0997 | - |
pH 7.4, 37°C | Homo sapiens | 4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol | |
| 0.109 | - |
pH 7.4, 37°C | Homo sapiens | 2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol | |
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Release 2023.1 (January 2023)
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