Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.146 extracted from

  • Veniant, M.M.; Hale, C.; Hungate, R.W.; Gahm, K.; Emery, M.G.; Jona, J.; Joseph, S.; Adams, J.; Hague, A.; Moniz, G.; Zhang, J.; Bartberger, M.D.; Li, V.; Syed, R.; Jordan, S.; Komorowski, R.; Chen, M.M.; Cupples, R.; Kim, K.W.; St Jean, D.J.; Johansson, L.; Henriksson, M.A.; Williams, M.; Vallgarda, J.; Fots, F.o.t.s.c.
    Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221) (2010), J. Med. Chem., 53, 4481-4487.
    View publication on PubMed
Search for more literature for 1.1.1.146

Inhibitors

Inhibitors Comment Organism Structure
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
 Homo sapiens
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
 Homo sapiens
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
 Homo sapiens
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
 Homo sapiens
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
 Homo sapiens
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
 Homo sapiens
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
 Homo sapiens
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
 Homo sapiens
2-(bicyclo[2.2.1]hept-2-ylamino)-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
-
 Homo sapiens
2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000012
-
 (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000128
-
 (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000173
-
 2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000278
-
 (S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000306
-
 (R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000472
-
 (R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.000058
-
 2-(bicyclo[2.2.1]hept-2-ylamino)-5-(propan-2-yl)-1,3-thiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.000227
-
 (S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.000329
-
 (R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.00077
-
 (R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one pH not specified in the publication, temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000101
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
0.0000126
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
0.0000153
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
0.0000286
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
0.0000568
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
0.000062
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
0.000885
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
0.000931
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
0.001505
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one