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Literature summary for 1.1.1.146 extracted from

  • Ryu, J.H.; Kim, S.; Han, H.Y.; Son, H.J.; Lee, H.J.; Shin, Y.A.; Kim, J.S.; Park, H.G.
    Synthesis and biological evaluation of picolinamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) (2015), Bioorg. Med. Chem. Lett., 25, 695-700.
    View publication on PubMed
Search for more literature for 1.1.1.146

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid
-
 Homo sapiens
3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid
-
 Homo sapiens
6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
 Homo sapiens
AMG-221
-
 Homo sapiens
AZD-4071
-
 Homo sapiens
BMS30
-
 Homo sapiens
Merck-544
-
 Homo sapiens
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide
-
 Homo sapiens
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide
-
 Homo sapiens
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide
-
 Homo sapiens
N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-cyclohexyl-6-(piperidin-1-yl)picolinamide
-
 Homo sapiens
N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
-
 Homo sapiens
PF-915275
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADPH + H+ Homo sapiens
-
 cortisol + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisone + NADPH + H+
-
 Homo sapiens cortisol + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
11beta-HSD1
-
 Homo sapiens
11beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000017
-
 at 37°C, pH not specified in the publication Homo sapiens N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide
0.0000018
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
0.0000019
-
 at 37°C, pH not specified in the publication Homo sapiens 6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000027
-
 at 37°C, pH not specified in the publication Homo sapiens N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide
0.0000028
-
 at 37°C, pH not specified in the publication Homo sapiens 6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000031
-
 at 37°C, pH not specified in the publication Homo sapiens 6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000032
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000032
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000037
-
 at 37°C, pH not specified in the publication Homo sapiens N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide
0.0000037
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
0.0000038
-
 at 37°C, pH not specified in the publication Homo sapiens N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
0.0000039
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000041
-
 at 37°C, pH not specified in the publication Homo sapiens 6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000046
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
0.0000064
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
0.0000066
-
 at 37°C, pH not specified in the publication Homo sapiens 6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000068
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
0.0000072
-
 at 37°C, pH not specified in the publication Homo sapiens N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
0.0000087
-
 at 37°C, pH not specified in the publication Homo sapiens 3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid
0.0000095
-
 at 37°C, pH not specified in the publication Homo sapiens N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide
0.000013
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
0.000018
-
 at 37°C, pH not specified in the publication Homo sapiens (1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid
0.000021
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
0.000027
-
 at 37°C, pH not specified in the publication Homo sapiens N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
0.000058
-
 at 37°C, pH not specified in the publication Homo sapiens N-cyclohexyl-6-(piperidin-1-yl)picolinamide