Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T24983 | Target Info | |||
Target Name | Dopamine D4 receptor (D4R) | ||||
Synonyms |
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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Target Type | Successful Target | ||||
Gene Name | DRD4 | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
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Compound Name |
Armodafinil
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Approved | Compound Info | ||
Synonyms |
Nuvigil; 112111-43-0; (R)-Modafinil; (R)-(-)-Modafinil; CEP-10953; UNII-V63XWA605I; CRL 40982; CEP 10953; V63XWA605I; CHEMBL1201192; CHEBI:77590; 2-[(R)-(Diphenylmethyl)sulfinyl]acetamide; (-)-2-((R)-(Diphenylmethyl)sulfinyl)acetamide; (-)-2-[(r)-(diphenylmethyl)sulfinyl]acetamide; Armodafinil [USAN:INN]; armodafinilo; armodafinilum; l-Modafinil; Nuvigil (TN); (-)-(R)-modafinil; Armodafinil (USAN/INN); SCHEMBL34489; ZINC6156; ACE037; Armodafinil, > YFGHCGITMMYXAQ-LJQANCHMSA-N
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Activity |
Ki ~ 100000 nM
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[1] | |||
Compound Name |
5-Propylamino-4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyridine-3-carboxylic acid methyl ester
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Investigative | Compound Info | ||
Synonyms |
CHEMBL383805; BDBM50172510
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Activity |
Ki = 90000 nM
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[2] | |||
Compound Name |
(2S)-4-(1H-Benzimidazol-2-ylmethyl)-2-(2-phenylethyl)morpholine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3335536; BDBM50027077
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Activity |
Ki ~ 100000 nM
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[3] | |||
Compound Name |
4-Methyl-5-[4-methyl-5-[3-[(2S,3R)-2-phenyl-5-azaspiro[2.4]heptan-5-yl]propylsulfanyl]-1,2,4-triazol-3-yl]-1,3-oxazole
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3983937; SCHEMBL17712767; BDBM50192034
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Activity |
Ki ~ 100000 nM
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[4] | |||
Compound Name |
CN1C(Scccn2ccoc(C2)C2=CC=C(C=C2)C(F)(F)F)=NN=C1C1=C(C)N=CO1
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3764557; SCHEMBL18741905; BDBM50139861
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Activity |
Ki ~ 100000 nM
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[5] |
Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
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Compound Name |
(4As,5R,10bR)-5-phenyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[h]isoquinoline-7,8-diol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1224527; BDBM50325822; trans-(5R)-5-phenyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[h]isoquinoline-7,8-diol
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Activity |
Ki = 2650000 nM
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[6] |
References | Top | ||||
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REF 1 | Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. J Med Chem. 2016 Dec 8;59(23):10676-10691. | ||||
REF 2 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of he... J Med Chem. 2005 Sep 8;48(18):5771-9. | ||||
REF 3 | Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity. ACS Med Chem Lett. 2014 Jul 9;5(9):1060-4. | ||||
REF 4 | 1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists. J Med Chem. 2016 Sep 22;59(18):8549-76. | ||||
REF 5 | Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1329-32. | ||||
REF 6 | Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists. Bioorg Med Chem. 2010 Sep 15;18(18):6763-70. |
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