Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T10897 | Target Info | |||
| Target Name | Acyl-CoA desaturase (SCD) | ||||
| Synonyms |
hSCD1; Stearoyl-coenzyme A (Delta9) desaturase; Stearoyl-CoA desaturase; Membrane-bound 9 desaturase; Fatty acid desaturase; DesA3; Des A3; Delta-9-stearoyl desaturase; Delta-9 desaturase; Delta(9)-desaturase; 9 stearoyl-desaturase
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| Target Type | Successful Target | ||||
| Gene Name | SCD | ||||
| Biochemical Class | Paired donor oxygen oxidoreductase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-[5-(2H-Tetrazol-5-yl)-1,3,4-thiadiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2153599; 1-[5-(2H-Tetrazol-5-yl)-1,3,4-thiadiazol-2-yl}-4-[2-(trifluoromethyl)phenoxy]piperidine; SCHEMBL473002; BDBM50393164; 2-(2H-tetrazol-5-yl)-5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(5-{2-[6-(2-Chloro-5-fluorophenyl)-2,6-diazaspiro[3.3]hept-2-yl]-1,3-thiazol-5-yl}-2H-tetrazol-2-yl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1938877; SCHEMBL1393669; BDBM50362589
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| Activity |
IC50 = 50900 nM
|
[2] | |||
| Compound Name |
2-[5-[5-[3-(2-Bromo-5-fluorophenoxy)propoxy]-1,3,4-thiadiazol-2-yl]tetrazol-2-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1950549; SCHEMBL13332587; BDBM50364039
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| Activity |
IC50 ~ 60000 nM
|
[3] | |||
| Compound Name |
2-(4-(2-(Trifluoromethyl)benzoyl)piperazin-1-yl)thiazole-5-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL569610; 2-{4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl}-1,3-thiazole-5-carboxylic acid; 2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxylic acid; SCHEMBL25775; KS-00000RNE; DTXSID60670440; BDBM50301059; MFCD13193184; ZINC45254195; AKOS022171766; ACN-025270; AK136242; AS-73146; SC-72518; DB-079150; FT-0720622
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| Activity |
IC50 = 68000 nM
|
[4] | |||
| Compound Name |
CID 46916597
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1938878; SCHEMBL1393948; BDBM50362590
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[5-[3-[2-[(2-Bromo-5-fluorophenyl)methoxy]ethoxy]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1950548; BDBM50364038
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
CID 46916547
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1938879; SCHEMBL1394428; BDBM50362591
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5-{2-[1-(3,4,5-Trichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1,3-thiazol-5-yl}-2H-tetrazolyl)acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1915556; SCHEMBL1985655; BDBM50356907; 2-[5-[2-[1-[(3,4,5-trichlorophenyl)methyl]triazol-4-yl]-1,3-thiazol-5-yl]tetrazol-2-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96. | ||||
| REF 2 | Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series. Bioorg Med Chem Lett. 2012 Jan 15;22(2):980-4. | ||||
| REF 3 | Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series. Bioorg Med Chem Lett. 2012 Jan 1;22(1):623-7. | ||||
| REF 4 | Thiazole analog as stearoyl-CoA desaturase 1 inhibitor. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5214-7. | ||||
| REF 5 | Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6505-9. | ||||
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