Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T99665 | Target Info | |||
| Target Name | GABA(A) receptor rho1 (GABRR1) | ||||
| Synonyms |
Gamma-aminobutyric acid receptor subunit rho-1; GABA(C) receptor1; GABA(A) receptor subunit rho-1
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| Target Type | Literature-reported Target | ||||
| Gene Name | GABRR1 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-(Aminomethyl)-1-hydroxypyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315213; BDBM50425647
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| Activity |
EC50 = 55000 nM
|
[1] | |||
| Compound Name |
(1S,2S)-2-(Aminomethyl)cyclopropanecarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL488308; ZINC4202476; BDBM50243927; 2beta-(Aminomethyl)cyclopropane-1alpha-carboxylic acid
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| Activity |
EC50 = 59000 nM
|
[2] | |||
| Compound Name |
Butanoic acid, 4-amino-2-methyl-, (2S)-
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL256608; SCHEMBL11924540; CTK2H1584; DTXSID20358974; ZINC518266; (S)-2-Methyl-4-aminobutyric acid; (s)-4-amino-2-methyl-butyric acid; BDBM50374647
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| Activity |
EC50 = 65000 nM
|
[3] | |||
| Compound Name |
(+)-cis-2-Aminomethylcyclopropane carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL230115; (1S,2R)-2-(Aminomethyl)Cyclopropanecarboxylic Acid; SCHEMBL340609; CTK1B9239; ZINC4202477; BDBM50241194; (1S,2R)-2-aminomethyl-cyclopropanecarboxylic acid; Q4540631; 2alpha-(Aminomethyl)-1alpha-cyclopropanecarboxylic acid; Cyclopropanecarboxylic acid, 2-(aminomethyl)-, (1S,2R)-; (1s,2r)-(+)-2-(aminomethyl)-cyclopropane-1-carboxylic acid
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| Activity |
EC50 = 68000 nM
|
[4] | |||
| Compound Name |
4-Amino-N-methoxycyclopentene-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2398122; BDBM50492305
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| Activity |
IC50 = 81500 nM
|
[5] | |||
| Compound Name |
4-Amino-N-prop-2-enoxycyclopentene-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2398114; BDBM50492302
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| Activity |
IC50 = 115300 nM
|
[5] | |||
| Compound Name |
4-Amino-N-ethoxycyclopentene-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2398123; BDBM50492299
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| Activity |
IC50 = 153000 nM
|
[5] | |||
| Compound Name |
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|
Compound Info | |||
| Activity |
IC50 = 62000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 14 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-Amino-N-methylcyclopentene-1-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2398116; BDBM50492301
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| Activity |
IC50 = 408300 nM
|
[5] | |||
| Compound Name |
(5-Chloro-1-hydroxypyrazol-4-yl)methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315214; BDBM50425646
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
(1-Hydroxy-5-methylpyrazol-4-yl)methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315216; BDBM50425645; ZINC95597547
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
(1-Hydroxy-3-phenylpyrazol-4-yl)methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315222; BDBM50425642
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
(3-Ethyl-1-hydroxypyrazol-4-yl)methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315220; BDBM50425643
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
(1-Hydroxy-3-iodopyrazol-4-yl)methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315218; BDBM50425644
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
[1-Hydroxy-3-(3-phenylphenyl)pyrazol-4-yl]methanamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2311576; BDBM50425641
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|
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
[1-Hydroxy-3-(4-phenylphenyl)pyrazol-4-yl]methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2315226; BDBM50425640
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|
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| Activity |
EC50 > 500000 nM
|
[1] | |||
| Compound Name |
4-Amino-N-propylcyclopentene-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2398117; BDBM50492300
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| Activity |
IC50 = 570000 nM
|
[5] | |||
| Compound Name |
cis-2-Aminocyclopropanecarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL257442; (1R,2S)-2-AMINOCYCLOPROPANE-1-CARBOXYLIC ACID; 2-aminocyclopropane carboxylic acid; SCHEMBL9512745; CTK2H6774; BDBM50374649; ZINC20363168; AKOS006359796; 2beta-Aminocyclopropane-1beta-carboxylic acid; Cyclopropanecarboxylicacid, 2-amino-, cis- (9CI)
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| Activity |
IC50 = 890000 nM
|
[3] | |||
| Compound Name |
6-Amino-2-ethylpyridine-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3322871; SCHEMBL2859498; BDBM50052794
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| Activity |
EC50 > 1000000 nM
|
[7] | |||
| Compound Name |
6-Amino-4-butylpyridine-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3322877; BDBM50052798
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| Activity |
EC50 > 1000000 nM
|
[7] | |||
| Compound Name |
6-Amino-2-butylpyridine-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3322872; BDBM50052795
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|
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| Activity |
EC50 > 1000000 nM
|
[7] | |||
| Compound Name |
6-Amino-4-ethylpyridine-3-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3322876; SCHEMBL2859500; BDBM50052797
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|
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| Activity |
EC50 > 1000000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as -aminobutyric acid(a) receptor agonists. J Med Chem. 2013 Feb 14;56(3):993-1006. | ||||
| REF 2 | Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships. J Med Chem. 2008 Jul 10;51(13):3825-40. | ||||
| REF 3 | Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):402-4. | ||||
| REF 4 | GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology. J Med Chem. 2000 Apr 20;43(8):1427-47. | ||||
| REF 5 | -aminobutyric acid(C) (GABAC) selective antagonists derived from the bioisosteric modification of 4-aminocyclopent-1-enecarboxylic acid: amides and hydroxamates. J Med Chem. 2013 Jul 11;56(13):5626-30. | ||||
| REF 6 | Novel Cyclic Phosphinic Acids as GABAC Receptor Antagonists: Design, Synthesis, and Pharmacology. ACS Med Chem Lett. 2010 Oct 19;2(1):11-6. | ||||
| REF 7 | Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists. Eur J Med Chem. 2014 Sep 12;84:404-16. | ||||
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