Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T86805 | Target Info | |||
| Target Name | HUMAN eukaryotic initiation factor-4A (eIF4A) | ||||
| Synonyms |
eIF-4A; ATP-dependent RNA helicase Eif4a
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| Gene Name | EIF4A1; EIF4A2; EIF4A3 | ||||
| Biochemical Class | eIF4A subfamily | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 40 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-{5-[(Z)-(2-Cyclohexyl-5-imino-7-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6(7H)-ylidene)methyl]-2-furyl}benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4092701; STK054791; ZINC13944002; AKOS001659417; SR-01000471906; SR-01000471906-1
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 = 57000 nM
|
[1] | ||
| Compound Name |
(R)-(4-(4-Bromobenzoyl)-3-(4-chlorophenyl)piperazin-1-yl)(6-bromopyrazolo[1,5-a]pyridin-3-yl)methanone
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|
Investigative | Compound Info | ||
| Synonyms |
eIF4A3 inhibitor, 3; CHEMBL4100633; BDBM65494; CS-0098463
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 = 60000 nM
|
[2] | ||
| Compound Name |
(4-Chlorophenyl)-[2-(4-chlorophenyl)-4-(1H-indazole-3-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4098513; BDBM50265563
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 = 62000 nM
|
[2] | ||
| Compound Name |
(4-Chlorophenyl)-[2-(4-chlorophenyl)-4-(2-phenyl-1,3-oxazole-4-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4096777; BDBM50265595
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 = 69000 nM
|
[2] | ||
| Compound Name |
4-(4-Chlorobenzoyl)-3-(4-chlorophenyl)-1-[(2-phenyl-1,3-oxazol-5-yl)methyl]piperazin-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4069442; BDBM50265576
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
6-Ethyl-1H-indole-2-carboxylic Acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4082138; SCHEMBL1144575; CTK6D1869; KS-00001LZR; ZINC3748674; BBL020926; BDBM50235742; MFCD02664480; STK893632; AKOS000118129; MCULE-2407272790; NCGC00338201-01; EN300-15107; K-8372; AB01329750-02; 6-Ethyl-1H-indole-2-carboxylic acid, AldrichCPR; Z199054778
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
(3S,3'R,5'S)-5-Fluoro-3'-methyl-1'-(1-methylimidazole-4-carbonyl)-5'-(2-methylpropyl)spiro[1H-indole-3,2'-pyrrolidine]-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4070683; BDBM50260390; J3.657.575A
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[4] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
6-Benzyl-3-[3-(pyridin-3-ylmethoxy)phenyl]-1,4-dihydropyrido[4,3-d]pyrimidine-2,7-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4097764
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[1] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(4-Chlorophenyl)-[2-(4-chlorophenyl)-4-(5-phenyl-1,3-oxazole-2-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4070581; BDBM50265570
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
(4-Chlorophenyl)-[2-(3-chlorophenyl)-4-(2-phenyl-1,3-oxazole-5-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4081199; BDBM50265577
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
7-Fluoro-6-propan-2-yl-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4061441; BDBM50235740
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
Chembl4175313
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50283445
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[5] | ||
| HUMAN eukaryotic initiation factor-4A II |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Eif4A3-IN-2
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|
Investigative | Compound Info | ||
| Synonyms |
eIF4A3 inhibitor, 2; CHEMBL4070071; BDBM65493; HY-101785; CS-0021895
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[5] | ||
| HUMAN eukaryotic initiation factor-4A II |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
(4-Chlorophenyl)-[2-(4-chlorophenyl)-4-(1-phenylpyrazole-3-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4060883; BDBM50265569
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
(3S,3'R,5'S)-1'-(1-Benzylimidazole-4-carbonyl)-5-fluoro-3'-methyl-5'-(2-methylpropyl)spiro[1H-indole-3,2'-pyrrolidine]-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4091579; BDBM50260424; J3.657.576J
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[4] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
Eif4A3-IN-1
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4073833; BDBM50265561; HY-101513; CS-0021616
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[2] | ||
| HUMAN eukaryotic initiation factor-4A II |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
6-Chloro-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
6-Chloroindole-2-carboxylic acid; 1H-Indole-2-carboxylic acid, 6-chloro-; CHEMBL23134; MFCD01863157; EINECS 240-799-5; PubChem1671; ACMC-209dwc; Oprea1_764381; SCHEMBL671001; CTK0H4790; 6-chloro-2-indolecarboxylic acid; DTXSID20168277; 6-chloro indole-2-carboxylic acid; ACT02557; BCP27306; ZINC2386971; ANW-22282; BBL020774; BDBM50235743; SBB066616; STK893464; AKOS000577202; MCULE-1413303202; AC-22702; AS-14992; BR-28859; SC-01590; AB0015827; DB-007146; BB 0248955; CS-0081874; FT-0601331; FT-0652327; ST50321553; EN300-15085; M-2317; 732C755; AE-861/30098019; ETHYL6-BROMO-2-METHYLQUINOLINE-4-CARBOXYLATE; W-107911; Z197512768
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
6-Benzyl-3-(3-phenylmethoxyphenyl)-1,4-dihydropyrido[4,3-d]pyrimidine-2,7-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4065018
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[1] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(3-Chlorophenyl)-[2-(4-chlorophenyl)-4-(2-phenyl-1,3-oxazole-5-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4067861; BDBM50265598
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
Methyl 6-isopropyl-1H-indole-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4062984; methyl 6-(propan-2-yl)-1H-indole-2-carboxylate; CTK6I9550; ZINC4235071; BBL021156; BDBM50235790; KM5189; MFCD06653516; STK893862; AKOS000123987; MCULE-6438642732; DA-43270; FT-0730485; 6-Isopropyl-1H-indole-2-carboxylic acid methyl ester
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
5-Isopropyl-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
5-propan-2-yl-1H-indole-2-carboxylic Acid; CHEMBL4071613; 1H-Indole-2-carboxylic acid, 5-(1-methylethyl)-; SCHEMBL3643479; CTK4H9707; DTXSID00407671; ZINC3748658; BDBM50235744; MFCD02664438; AKOS001476621; AK-42181; AS-18330; DA-37247; AB0000695; BB 0248946; FT-0660074; W5909; 5-(propan-2-yl)-1H-indole-2-carboxylic acid; S-1117
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
6-Benzyl-3-(3-(thiazol-5-ylmethoxy)phenyl)-3,4-dihydropyrido[4,3-d]pyrimidine-2,7(1H,6H)-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4084949
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[1] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
7-Chloro-6-propan-2-yl-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4089574; BDBM50235797
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
7-Isopropyl-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
7-propan-2-yl-1H-indole-2-carboxylic Acid; CHEMBL4075940; CTK4H9705; DTXSID30405261; KS-00000RD6; ZINC3748654; 4946AB; BDBM50235789; MFCD02664430; AKOS001476421; CS-W006884; AK-93304; AS-63982; 7-(propan-2-yl)-1H-indole-2-carboxylic acid; S-1315
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
(4-Chlorophenyl)-[2-(4-chlorophenyl)-4-(2-phenyl-1,3-oxazole-5-carbonyl)-1,4-diazepan-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4073307; BDBM50265597
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
Chembl4170030
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Investigative | Compound Info | ||
| Synonyms |
BDBM50283443
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|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[5] | ||
| HUMAN eukaryotic initiation factor-4A II |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
[3-(4-Chlorophenyl)-4-[(4-chlorophenyl)methyl]piperazin-1-yl]-(2-phenyl-1,3-oxazol-5-yl)methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4099221; BDBM50265575
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
6-Propan-2-yl-1H-indole-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4084655; BDBM50235791
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
6-Benzyl-3-[2-(3-fluoropyridin-2-yl)-6-methyl-3,4-dihydro-2H-chromen-7-yl]-1,4-dihydropyrido[4,3-d]pyrimidine-2,7-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4087449
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|
||||
| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[1] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(4-Chlorophenyl)-[2-(4-chlorophenyl)-4-[(2-phenyl-1,3-oxazol-5-yl)methyl]piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4081198; BDBM50265596
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
(2-Chlorophenyl)-[2-(4-chlorophenyl)-4-(2-phenyl-1,3-oxazole-5-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4061955; BDBM50265587
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
(4-Chlorophenyl)-[2-(2-chlorophenyl)-4-(2-phenyl-1,3-oxazole-5-carbonyl)piperazin-1-yl]methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4105452; BDBM50265578
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
1-Methyl-6-(1-methylethyl)-1H-indole-2-carboxylic Acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4074367; 1-Methyl-6-(propan-2-yl)-1H-indole-2-carboxylic acid; 6-Isopropyl-1-methyl-1H-indole-2-carboxylic acid; SCHEMBL13895693; KS-00001M0Z; BDBM50235793; MFCD16810548; ZINC71976869; J-005037
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
6-Methyl-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
6-Methylindole-2-carboxylic acid; 1H-Indole-2-carboxylicacid, 6-methyl-; CHEMBL596007; SCHEMBL1144688; CTK0H2206; KS-00000FGK; DTXSID70390349; HMS1630E02; ACT09171; ALBB-032679; ZINC2582714; ANW-48397; BBL020943; BDBM50305666; MFCD02664477; SBB010573; STK893649; AKOS000118128; FS-2410; MCULE-8264158205; SB15196; NCGC00337851-01; AK-77187; BR-77187; SC-20916; 6-METHYL INDOLE-2-CARBOXYLIC ACID; AB0001750; 6-METHYL-1H-INDOLE-2-CARBOXYLICACID; BB 0216437; CS-0018975; FT-0677786; ST50294005; W3994; EN300-15104; S-5444; AB01329949-02; 6-Methyl-1H-indole-2-carboxylic acid, AldrichCPR; J-518910; Q27454576; Z197513748
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|
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| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
(3R,3'S,5'R)-1'-(1-Benzylimidazole-4-carbonyl)-5-fluoro-3'-methyl-5'-(2-methylpropyl)spiro[1H-indole-3,2'-pyrrolidine]-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4073413; BDBM50260426
Click to Show/Hide
|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[4] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
(4-Chlorophenyl)-[2-cyclohexyl-4-(2-phenyl-1,3-oxazole-5-carbonyl)piperazin-1-yl]methanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4089076; BDBM50265586
Click to Show/Hide
|
||||
| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
4-Chloro-6-propan-2-yl-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4099717; BDBM50235741
Click to Show/Hide
|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
3-[4-[(3R)-4-(4-Bromobenzoyl)-3-(4-chlorophenyl)piperazine-1-carbonyl]-5-methylpyrazol-1-yl]benzonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4100039; BDBM50265558
Click to Show/Hide
|
||||
| Activity | HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[2] | ||
| Compound Name |
(3R,3'S,5'R)-5-Fluoro-3'-methyl-1'-(1-methylimidazole-4-carbonyl)-5'-(2-methylpropyl)spiro[1H-indole-3,2'-pyrrolidine]-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4099313; BDBM50260425
Click to Show/Hide
|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[4] | ||
| HUMAN eukaryotic initiation factor-4A III |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
4-Chloro-6-isopropyl-7-fluoro-1H-indole-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4070102; BDBM50235737; J3.639.766G; 4-chloro-7-fluoro-6-isopropyl-1h-indole-2-carboxylic acid
Click to Show/Hide
|
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| Activity | HUMAN eukaryotic initiation factor-4A I |
IC50 ~ 100000 nM
|
[3] | ||
| HUMAN eukaryotic initiation factor-4A II |
IC50 ~ 100000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2. J Med Chem. 2017 Jul 13;60(13):5759-5771. | ||||
| REF 2 | Discovery of Novel 1,4-Diacylpiperazines as Selective and Cell-Active eIF4A3 Inhibitors. J Med Chem. 2017 Apr 27;60(8):3335-3351. | ||||
| REF 3 | Discovery of selective ATP-competitive eIF4A3 inhibitors. Bioorg Med Chem. 2017 Apr 1;25(7):2200-2209. | ||||
| REF 4 | Discovery of spiro[indole-3,2'-pyrrolidin]-2(1H)-one based inhibitors targeting Brr2, a core component of the U5 snRNP. Bioorg Med Chem. 2017 Sep 1;25(17):4753-4767. | ||||
| REF 5 | Discovery of Novel 5-(Piperazine-1-carbonyl)pyridin-2(1 H)-one Derivatives as Orally eIF4A3-Selective Inhibitors. ACS Med Chem Lett. 2017 Sep 8;8(10):1077-1082. | ||||
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