| Reaction Details |
|---|
| Report a problem with these data |
| Target | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) |
|---|
| Ligand | N-(Pyridin-2-yl) arylsulfonamide, 26 |
|---|
| Substrate/Competitor | [3H]-cortisone |
|---|
| Meas. Tech. | Measurement of 11beta-HSD1 Activity |
|---|
| pH | 8±n/a |
|---|
| Temperature | 295.15±n/a K |
|---|
| Ki | <1±n/a nM |
|---|
| Citation |  Siu, M; Johnson, TO; Wang, Y; Nair, SK; Taylor, WD; Cripps, SJ; Matthews, JJ; Edwards, MP; Pauly, TA; Ermolieff, J; Castro, A; Hosea, NA; LaPaglia, A; Fanjul, AN; Vogel, JE N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.Bioorg Med Chem Lett.19:3493-7(2009)[PubMed] |
|---|
| More Info. |
Get all data from this article
, Solution Info
, Assay Method
|
|---|
| 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) |
|---|
| Name | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) |
|---|
| Synonyms | 11-DH | Corticosteroid 11-beta-dehydrogenase isozyme 1 | EC 1.1.1.146 |
|---|
| Type | Homodimer; oxidoreductase |
|---|
| Mol. Mass. | n/a |
|---|
| Organism | Homo sapiens (human) |
|---|
| Description | The sequence for the truncated form of human 11beta-HSD1 (24-292) was cloned and expressed in E. coli. The purified protein was used in enzyme assays. |
|---|
| Residue | 269 |
|---|
| Sequence | NEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTARSKETLQKVVSHCLELGA
ASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSLNLFHDDIHHVRKSMEVN
FLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSASKFALDGFFSSIRKEYSV
SRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEIIKGGALRQEEVYYDSSLW
TTLLIRNPCRKILEFLYSTSYNMDRFINK
| |
|
|---|
| N-(Pyridin-2-yl) arylsulfonamide, 26 |
|---|
| Name | N-(Pyridin-2-yl) arylsulfonamide, 26 |
|---|
| Synonyms: | n/a |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C18H14N4O2S |
|---|
| Mol. Mass. | 350.394 |
|---|
| SMILES | Nc1cccc(NS(=O)(=O)c2ccc(cc2)-c2ccc(cc2)C#N)n1 |
|---|
| Structure | |
|---|
| [3H]-cortisone |
|---|
| Name | [3H]-cortisone |
|---|
| Synonyms: | (1S,2R,10S,11S,14R,15S)-14-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-ene-5,17-dione |
|---|
| Type | radiolabeled substrate |
|---|
| Emp. Form. | C21H28O5 |
|---|
| Mol. Mass. | 360.444 |
|---|
| SMILES | [H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)CC(=O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C |t:23| |
|---|
| Structure | |
|---|