Reaction Details
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11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50054691
Substrate
n/a
Meas. Tech.
ChEMBL_1453118 (CHEMBL3364416)
IC50
1.6±n/a nM
Citation
Li, J; Kennedy, LJ; Wang, H; Li, JJ; Walker, SJ; Hong, Z; O'Connor, SP; Nayeem, A; Camac, DM; Morin, PE; Sheriff, S; Wang, M; Harper, T; Golla, R; Seethala, R; Harrity, T; Ponticiello, RP; Morgan, NN; Taylor, JR; Zebo, R; Gordon, DA; Robl, JA Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1). ACS Med Chem Lett 5:803-8 (2014) [PubMed] Article More 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:
BDBM50054691
Synonyms:
CHEMBL3318978
Type:
Small organic molecule
Emp. Form.:
C18H16ClN3
Mol. Mass.:
309.793
SMILES:
Clc1ccc(cc1)C1(CC1)c1nnc2c(cccn12)C1CC1
Structure:
