Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T97537 | Target Info | |||
| Target Name | Leucyl-cysteinyl aminopeptidase (LNPEP) | ||||
| Synonyms |
Placental leucine aminopeptidase; P-LAP; Oxytocinase; OTase; Leucyl-cystinyl aminopeptidase; Insulin-responsive aminopeptidase; Insulin-regulated membrane aminopeptidase; IRAP; Cystinyl aminopeptidase
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| Target Type | Patented-recorded Target | ||||
| Gene Name | LNPEP | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 19 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Methyl 4-amino-3-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]benzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416566; BDBM50076745
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| Activity |
IC50 = 57000 nM
|
[1] | |||
| Compound Name |
Methyl (2S)-6-amino-2-[[3-amino-4-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]benzoyl]amino]hexanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416718; BDBM50076983
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| Activity |
IC50 = 70000 nM
|
[1] | |||
| Compound Name |
(2S,3R)-2-(3-(4-Hydroxybenzyl)-5-((S)-2-amino-3-methylbutanamido)benzamido)-3-methylpentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL487435; BDBM50243086
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| Activity |
Ki = 76000 nM
|
[2] | |||
| Compound Name |
(S)-2-(2-((3-(4-Hydroxybenzyl)-5-(2-amino-3-methylbutanamido)benzamido)methyl)phenyl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL470072; BDBM50242938
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| Activity |
Ki = 86000 nM
|
[2] | |||
| Compound Name |
2-(2-(((2S,3R)-2-(3-(4-Hydroxybenzyl)-5-aminobenzamido)-3-methylpentanamido)methyl)phenyl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL469484; BDBM50242872
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| Activity |
Ki = 97000 nM
|
[2] | |||
| Compound Name |
2-(2-((3-(4-Hydroxybenzyl)-5-aminobenzamido)methyl)phenyl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL488627; BDBM50243085
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| Activity |
Ki ~ 100000 nM
|
[2] | |||
| Compound Name |
(2S)-5-Amino-2-[[4-amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl]amino]pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416576; BDBM50077131
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-2-[[4-Amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl]amino]-3-methylbutanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2420379; BDBM50439356
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
(2S)-2-[[4-Amino-3-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]benzoyl]amino]-3-(1H-indol-3-yl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416686; BDBM50077023
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-2-[[4-Amino-3-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]benzoyl]amino]-3-methylbutanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416587; BDBM50076966
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-2-[(3,4-Diaminobenzoyl)amino]-3-(1H-indol-3-yl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416706; BDBM50076975
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Methyl (2S)-6-amino-2-[[4-amino-3-[[(2S)-2-aminohexanoyl]amino]benzoyl]amino]hexanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416584; BDBM50076962
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Methyl (2S)-6-amino-2-[(3,4-diaminobenzoyl)amino]hexanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416703; BDBM50076974
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-2-[[3-Amino-4-[[(2S)-2-aminohexanoyl]amino]benzoyl]amino]-3-methylbutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416724; BDBM50077122
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Ethyl 2-amino-4-(4-chlorophenyl)-7-hydroxy-4H-chromene-3-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3125939; CBMicro_038545; Oprea1_456803; Oprea1_765838; DTXSID00397088; STK860394; AKOS005609535; MCULE-4735499673; BIM-0038562.P001; ethyl 2-amino-4-(4-chlorophenyl)-7-hydroxy-4 h -chromene-3-carboxylate
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| Activity |
Ki ~ 100000 nM
|
[4] | |||
| Compound Name |
Methyl (2S)-6-amino-2-[[3-amino-4-[[(2S)-2-amino-4-methylpentanoyl]amino]benzoyl]amino]hexanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416722; BDBM50077132
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-2-[[4-Amino-3-[[(2S)-2-aminohexanoyl]amino]benzoyl]amino]-3-methylbutanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416690; BDBM50077030
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Methyl (2S,3R)-2-[[4-amino-3-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]benzoyl]amino]-3-hydroxybutanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3416589; BDBM50076968
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-Amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2420387; BDBM50439348
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 3,4-diaminobenzoic acid derivatives as inhibitors of the oxytocinase subfamily of M1 aminopeptidases with immune-regulating properties. J Med Chem. 2015 Feb 12;58(3):1524-43. | ||||
| REF 2 | Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2. Bioorg Med Chem. 2008 Jul 15;16(14):6924-35. | ||||
| REF 3 | Novel selective inhibitors of aminopeptidases that generate antigenic peptides. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4832-6. | ||||
| REF 4 | Synthesis, structure-activity relationships and brain uptake of a novel series of benzopyran inhibitors of insulin-regulated aminopeptidase. J Med Chem. 2014 Feb 27;57(4):1368-77. | ||||
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