Reaction Details 
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11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50356451
Substrate
n/a
Meas. Tech.
ChEMBL_775553 (CHEMBL1913237)
IC50
3±n/a nM
Citation
Wu, SC; Yoon, D; Chin, J; van Kirk, K; Seethala, R; Golla, R; He, B; Harrity, T; Kunselman, LK; Morgan, NN; Ponticiello, RP; Taylor, JR; Zebo, R; Harper, TW; Li, W; Wang, M; Zhang, L; Sleczka, BG; Nayeem, A; Sheriff, S; Camac, DM; Morin, PE; Everlof, JG; Li, YX; Ferraro, CA; Kieltyka, K; Shou, W; Vath, MB; Zvyaga, TA; Gordon, DA; Robl, JA Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11ß-hydroxydehydrogenase 1 (11ß-HSD1). Bioorg Med Chem Lett 21:6693-8 (2011) [PubMed] ArticleMore Info.:
Target
Name:
11-beta-hydroxysteroid dehydrogenase 1
Synonyms:
11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 1 (11HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11beta-HSD1) | DHI1_HUMAN | HSD11 | HSD11B1 | HSD11L | SDR26C1
Type:
Enzyme
Mol. Mass.:
32409.16
Organism:
Homo sapiens (Human)
Description:
P28845
Residue:
292
Sequence:
MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
Inhibitor
Name:
BDBM50356451
Synonyms:
CHEMBL1911695
Type:
Small organic molecule
Emp. Form.:
C17H15ClN2O2
Mol. Mass.:
314.766
SMILES:
Clc1ccccc1COc1[nH]c(=O)c(C#N)c2CCCCc12
Structure:
