Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T29683 | Target Info | |||
| Target Name | Neuromedin-K receptor (TACR3) | ||||
| Synonyms |
Tachykinin receptor 3; TACR3; Neuromedin K receptor; Neurokinin-3 receptor; Neurokinin B receptor; NKR; NK-3R; NK-3 receptor
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| Target Type | Successful Target | ||||
| Gene Name | TACR3 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 4 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(4S)-4-(3-Ethoxy-4-hydroxy-5-nitrophenyl)-5-phenyl-6-pyridin-3-yl-3,4-dihydro-1H-pyrimidin-2-one
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1516350; CHEMBL3650417; BDBM140264
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| Activity |
IC50 = 55000 nM
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[1] | |||
| Compound Name |
(E)-1-[4-[(4-Chlorophenyl)-phenylmethyl]piperazin-1-yl]-3-phenylprop-2-en-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL95489; BDBM50283773; (E)-1-{4-[(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-yl}-3-phenyl-propenone
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| Activity |
IC50 = 60000 nM
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[2] | |||
| Compound Name |
2-[[(2S)-2-[[(2S)-2-Amino-3-phenylpropanoyl]-methylamino]-3-phenylpropanoyl]amino]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3361403; BDBM50028020
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| Activity |
EC50 ~ 100000 nM
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[3] | |||
| Compound Name |
(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-Amino-3-phenylpropanoyl]-methylamino]-3-phenylpropanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3361402; BDBM50028019
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
n-Benzyl-7-methoxy-2-phenylquinoline-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL51120; SCHEMBL6450481; BDBM50051296; 7-Methoxy-2-phenyl-quinoline-4-carboxylic acid benzylamide
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| Activity |
Ki = 533000 nM
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[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | US patent application no. 8906933B2, Dihydropyrimidin-2(1H)-one compounds as neurokinin-3 receptor antagonists | ||||
| REF 2 | Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening.. Bioorg Med Chem Lett. 1994 Dec 22;4(24):2821-4. | ||||
| REF 3 | Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation. J Med Chem. 2014 Oct 23;57(20):8646-51. | ||||
| REF 4 | 2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor. J Med Chem. 1996 Jun 7;39(12):2281-4. | ||||
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