Literature summary for 1.14.19.1 extracted from

Isabel, E.; Powell, D.A.; Black, W.C.; Chan, C.C.; Crane, S.; Gordon, R.; Guay, J.; Guiral, S.; Huang, Z.; Robichaud, J.; Skorey, K.; Tawa, P.; Xu, L.; Zhang, L.; Oballa, R.
Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors (2011), Bioorg. Med. Chem. Lett., 21, 479-483.

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Inhibitors

Inhibitors	Comment	Organism
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol	-	Homo sapiens
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol	-	Rattus norvegicus
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol	-	Homo sapiens
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol	-	Rattus norvegicus
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine	-	Homo sapiens
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine	-	Rattus norvegicus
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[3-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine	-	Rattus norvegicus
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine	-	Homo sapiens
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine	-	Rattus norvegicus
3-[3-(2,6-dichloro-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Homo sapiens
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Homo sapiens
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Homo sapiens
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
3-[3-(2-chloro-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Homo sapiens
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
3-[3-[2-chloro-3-(trifluoromethyl)phenoxy]azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine	-	Rattus norvegicus
[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol	-	Homo sapiens
[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol	-	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Rattus norvegicus	-	-	-

Synonyms

Synonyms	Comment	Organism
stearoyl-CoA desaturase	-	Homo sapiens
stearoyl-CoA desaturase	-	Rattus norvegicus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.0000023	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
0.0000023	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
0.0000034	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
0.0000049	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
0.0000056	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
0.0000072	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000009	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
0.000013	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
0.000019	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000021	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
0.000021	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000022	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000023	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000027	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
0.000028	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.00004	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.00005	-	HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
0.000067	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000163	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-(2-chloro-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.001992	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[3-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
0.003385	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-[2-chloro-3-(trifluoromethyl)phenoxy]azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.008167	-	rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	3-[3-(2,6-dichloro-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine