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Target
Alpha-2C adrenergic receptor
Ligand
BDBM643051
Substrate
n/a
Meas. Tech.
In Vitro Radioligand Binding Assay
IC50
0.540±n/a nM
Citation
 DELBECK, M; HAHN, M COMBINATION OF AN ALPHA2-ADRENOCEPTOR SUBTYPE C (ALPHA-2C) ANTAGONIST WITH A TASK1/3 CHANNEL BLOCKER FOR THE TREATMENT OF SLEEP APNEA US Patent  US20240000767 Publication Date 1/4/2024 
Target
Name:
Alpha-2C adrenergic receptor
Synonyms:
ADA2C_HUMAN | ADRA2C | ADRA2L2 | ADRA2RL2 | Adrenergic alpha2C | Adrenergic receptor | Adrenergic receptor alpha | Adrenergic, alpha-2C-, receptor | Alpha-2 adrenergic receptor subtype C4 | Alpha-2C adrenoceptor | Alpha-2C adrenoreceptor | adrenergic, alpha-2C-, receptor [Homo sapiens]
Type:
Enzyme
Mol. Mass.:
49552.32
Organism:
Homo sapiens (Human)
Description:
P18825
Residue:
462
Sequence:
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGFLIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFGQVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISAVISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLRTRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGALRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRRRRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFKFFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
  
Inhibitor
Name:
BDBM643051
Synonyms:
N-[(3,5-Difluoropyridin-2-yl)methyl]-4-ethyl-2-[(3R)-3-methyl[1,4′-bipiperidin]-1′-yl]-1,3-thiazole-5-carboxamide | US20240000767, Example 130
Type:
Small organic molecule
Emp. Form.:
C23H31F2N5OS
Mol. Mass.:
463.587
SMILES:
CCc1nc(sc1C(=O)NCc1ncc(F)cc1F)N1CCC(CC1)N1CCC[C@@H](C)C1 |r|
Structure:
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