Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31186 | Target Info | |||
| Target Name | Eukaryotic initiation factor 4E (EIF4E) | ||||
| Synonyms |
eIF4F 25 kDa subunit; eIF4E; eIF-4F 25 kDa subunit; eIF-4E; Eukaryotic translation initiation factor 4E; EIF4F; EIF4EL1
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|
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| Target Type | Literature-reported Target | ||||
| Gene Name | EIF4E | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 27 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Disodium;[(2R,3S,4R,5R)-5-(2-amino-7-methyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate;bromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351035
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|
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
(2Z)-2-[(7,8-Dimethoxy-4H-chromeno[4,3-d][1,3]thiazol-2-yl)hydrazinylidene]-3-(2-nitrophenyl)propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3287131; BDBM50018928
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|
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| Activity |
IC50 = 51500 nM
|
[2] | |||
| Compound Name |
[(2R,3S,4R,5R)-5-[2-Amino-7-[(2-chlorophenyl)methyl]-6-oxo-1H-purin-9-ium-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095941; BDBM50316309
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|
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| Activity |
IC50 = 54500 nM
|
[3] | |||
| Compound Name |
Sodium;[(2R,3R,4R,5R)-5-(2-amino-7-methyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-oxido-oxophosphanium
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3350705
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| Activity |
IC50 = 55000 nM
|
[1] | |||
| Compound Name |
4'-Chloro-4-[4-(3,4-dichloro-phenyl)-thiazol-2-yl]-2'-fluoro-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3663614; SCHEMBL14797080; BDBM167383; US9073881, 135; 2-(4-chloro-2-fluorophenyl)-5-[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]benzoic acid
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| Activity |
IC50 = 55000 nM
|
[4] | |||
| Compound Name |
(2Z)-2-[(6,7-Dimethoxy-4H-chromeno[4,3-d][1,3]thiazol-2-yl)hydrazinylidene]-3-(2-nitrophenyl)propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3287129; BDBM50018934
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|
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| Activity |
IC50 = 55500 nM
|
[2] | |||
| Compound Name |
[(2R,3S,4R,5R)-5-[2-Amino-7-[(3-chlorophenyl)methyl]-6-oxo-1H-purin-9-ium-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1097199; BDBM50316308
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|
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| Activity |
IC50 = 56800 nM
|
[3] | |||
| Compound Name |
Sodium;2-amino-7-(cyclodecapentaenylmethyl)-9-[(2R,3R,4R,5R)-5-(phosphooxymethyl)-3,4-di(propan-2-yloxy)oxolan-2-yl]purin-9-ium-6-olate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2367724
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|
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| Activity |
IC50 = 70000 nM
|
[1] | |||
| Compound Name |
4-[4-(3,4-Dichloro-phenyl)-thiazol-2-yl]-4'-(2-dimethylamino-ethylcarbamoyl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659407; SCHEMBL14797210; BDBM167300; US9073881, 49
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(3,4-Dichloro-phenyl)-thiazol-2-yl]-4'-(4-methyl-piperazine-1-carbonyl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3639582; SCHEMBL14797075; BDBM167304; US9073881, 53; 5-[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]-2-[4-(4-methylpiperazine-1-carbonyl)phenyl]benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
2'-Nitro-4-(4-pyridin-4-yl-thiazol-2-yl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659397; SCHEMBL14797202; BDBM167290; US9073881, 39; 2-(2-nitrophenyl)-5-(4-pyridin-4-yl-1,3-thiazol-2-yl)benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
2'-Nitro-4-(4-pyridin-3-yl-thiazol-2-yl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659396; SCHEMBL14797561; BDBM167289; US9073881, 38; 2-(2-nitrophenyl)-5-(4-pyridin-3-yl-1,3-thiazol-2-yl)benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(3,4-Dichloro-phenyl)-thiazol-2-yl]-4'-(2-morpholin-4-yl-ethylcarbamoyl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659416; SCHEMBL14797417; BDBM167310; US9073881, 59
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
2',3',5'-Trichloro-4-[4-(3,4-dichloro-phenyl)-thiazol-2-yl]-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3663627; SCHEMBL14797238; BDBM167397; US9073881, 149; 5-[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]-2-(2,3,5-trichlorophenyl)benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(2,6-Difluoro-phenyl)-thiazol-2-yl]-2'-nitro-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659378; SCHEMBL14797481; BDBM167271; US9073881, 20; 5-[4-(2,6-difluorophenyl)-1,3-thiazol-2-yl]-2-(2-nitrophenyl)benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(3,4-Dichloro-phenyl)-thiazol-2-yl]-4'-(1-methyl-piperidin-4-ylcarbamoyl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659409; SCHEMBL14797126; BDBM167302; US9073881, 51
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(3,4-Dichloro-phenyl)-thiazol-2-yl]-4'-(3-morpholin-4-yl-propylcarbamoyl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659415; SCHEMBL14797255; BDBM167309; US9073881, 58
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(4-Methanesulfonyl-phenyl)-thiazol-2-yl]-2'-nitro-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659391; SCHEMBL14797276; BDBM167284; US9073881, 33; 5-[4-(4-methylsulfonylphenyl)-1,3-thiazol-2-yl]-2-(2-nitrophenyl)benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
5-[4-(3,4-Dichlorophenyl)-1,3-thiazol-2-yl]-2-[4-[3-[ethyl(methyl)amino]propylcarbamoyl]phenyl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659406; SCHEMBL14806778; BDBM167299; US9073881, 48
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
4-[4-(3,4-Dichloro-phenyl)-thiazol-2-yl]-4'-(3-diethylamino-propylcarbamoyl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659405; SCHEMBL14797045; BDBM167298; US9073881, 47
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|
||||
| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
2'-Nitro-4-(4-pyridin-2-yl-thiazol-2-yl)-biphenyl-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3659395; SCHEMBL14797314; BDBM167288; US9073881, 37; 2-(2-nitrophenyl)-5-(4-pyridin-2-yl-1,3-thiazol-2-yl)benzoic acid
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|
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| Activity |
IC50 ~ 80000 nM
|
[4] | |||
| Compound Name |
Sodium;2-amino-7-benzyl-9-[(2R,3R,4R,5R)-5-(phosphooxymethyl)-3,4-di(propan-2-yloxy)oxolan-2-yl]purin-9-ium-6-olate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2367725
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|
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| Activity |
IC50 = 85000 nM
|
[1] | |||
| Compound Name |
[(2R,3S,4R,5R)-5-[2-Amino-7-[2-(4-chloroanilino)-2-oxoethyl]-6-oxo-1H-purin-9-ium-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2046911; BDBM50386770
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|
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| Activity |
IC50 = 85400 nM
|
[3] | |||
| Compound Name |
Disodium;[(2R,3S,4R,5R)-5-(2-amino-7-ethyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate;bromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351036
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|
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
Sodium;[(2R,3S,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxido-oxophosphanium
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3392215
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|
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| Activity |
IC50 = 130000 nM
|
[1] | |||
| Compound Name |
[(2R,3R,4R,5R)-5-(2-Amino-6-oxo-1H-purin-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-hydroxy-oxophosphanium;N,N-diethylethanamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351039
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|
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| Activity |
IC50 = 180000 nM
|
[1] | |||
| Compound Name |
Sodium;[(2R,3S,4R,5R)-5-(2-amino-7-benzyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxido-oxophosphanium;bromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3392213
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|
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| Activity |
IC50 = 200000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 20 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Disodium;[(2R,3S,4R,5R)-5-(2-amino-7-benzyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate;bromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351037
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|
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| Activity |
IC50 = 220000 nM
|
[1] | |||
| Compound Name |
Disodium;[(2R,3S,4R,5R)-5-(2-amino-6-oxo-7-prop-2-enyl-1H-purin-9-ium-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate;bromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351030
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|
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| Activity |
IC50 = 220000 nM
|
[1] | |||
| Compound Name |
7-[2-(4-Chlorophenoxy)ethyl]-8-(4-diethoxyphosphorylphenyl)-2-(methylamino)-1H-purin-6-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2046919; BDBM50386778
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|
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| Activity |
IC50 = 300000 nM
|
[3] | |||
| Compound Name |
Chembl4203412
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50452630
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|
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| Activity |
Ki = 382000 nM
|
[5] | |||
| Compound Name |
6-Mercapto-7-methylguanosine
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|
Investigative | Compound Info | ||
| Synonyms |
UNII-5F1954X1MN; 7-Methyl-6-thioguanosine; 5F1954X1MN; 7-methylthioguanosine; 2-Amino-6-mercapto-7-methylpurine ribonucleoside; CHEMBL1234483; 7-Methyl-6-thioguanosine chloride; Q27261945; 2-amino-7-methyl-9-beta-D-ribofuranosyl-9H-purin-7-ium-6-thiolate
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
Disodium;2-[[[(2R,3R,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-oxidophosphoryl]amino]acetate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2367487
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
[(2R,3R,4R,5R)-5-(2-Amino-7-methyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methanolate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3350707
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
9-[(2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-[(4-methylphenyl)sulfanylamino]-1H-purin-6-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351038
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
2-Amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-methyl-1H-purin-9-ium-6-one;bromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351034
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
[(2R,3R,4R,5R)-5-(2-Amino-7-benzyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methanolate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3350708
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
Disodium;2-[[[(2R,3R,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-oxidophosphoryl]amino]-3-(1H-indol-3-yl)propanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2367484
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
[(2R,3R,4R,5R)-5-(2-Amino-7-ethyl-6-oxo-1H-purin-9-ium-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methanolate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3350706
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
2'-Deoxyguanosine 5'-(tetrasodium triphosphate)
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|
Investigative | Compound Info | ||
| Synonyms |
EINECS 277-810-8; CHEMBL2368456; DTXSID80225310; AKOS025312543
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
Disodium;2-[[[(2R,3R,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-oxidophosphoryl]amino]-3-oxo-3-phenylpropanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2367485
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|
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| Activity |
IC50 = 400000 nM
|
[1] | |||
| Compound Name |
2-Methylguanosine
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|
Investigative | Compound Info | ||
| Synonyms |
N2-Methylguanosine; N(2)-Methylguanosine; N-methylguanosine; Guanosine, N-methyl-; UNII-45T7B5IAN4; 45T7B5IAN4; n-methyl-Guanosine; N-Methyl guanosine; N2-Methylguanine riboside; SCHEMBL41509; CHEMBL3351027; CTK1A0934; DTXSID20943960; MFCD00057039; ZINC12496640; HY-111647; CS-0089200; J-014035; Q1419713; 2-(Methylimino)-9-pentofuranosyl-3,9-dihydro-2H-purin-6-ol; 2-(methylamino)-9-(beta-D-ribofuranosyl)-1,9-dihydro-6H-purin-6-one
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|
||||
| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
9-[(2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,7-dimethylpurin-9-ium-6-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351029
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
Sodium;[(2R,3R,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-[(1-methoxy-1-oxo-3-phenylpropan-2-yl)amino]phosphinate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2021409
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|
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
Disodium;3-[[[(2R,3R,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-di(propan-2-yloxy)oxolan-2-yl]methoxy-oxidophosphoryl]amino]propanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2367486
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|
||||
| Activity |
IC50 = 400000 nM
|
[1] | |||
| Compound Name |
7-[(2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-(dimethylamino)-3H-pyrrolo[2,3-d]pyrimidin-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3351033
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|
||||
| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
2'-O,3'-O-Diisopropylguanosine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2368460
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|
||||
| Activity |
IC50 > 400000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and evaluation of potential inhibitors of eIF4E cap binding to 7-methyl GTP. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2177-80. | ||||
| REF 2 | Synthesis of rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) mimetic and their in vitro characterization as inhibitors of protein-protein interaction. J Med Chem. 2014 Jun 26;57(12):5094-111. | ||||
| REF 3 | Structure-guided design, synthesis, and evaluation of guanine-derived inhibitors of the eIF4E mRNA-cap interaction. J Med Chem. 2012 Apr 26;55(8):3837-51. | ||||
| REF 4 | US patent application no. 9073881B2, Benzoic acid derivatives | ||||
| REF 5 | 7-Methylguanosine monophosphate analogues with 5'-(1,2,3-triazoyl) moiety: Synthesis and evaluation as the inhibitors of cNIIIB nucleotidase. Bioorg Med Chem. 2018 Jan 1;26(1):191-199. | ||||
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