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Target
Alpha-2A adrenergic receptor
Ligand
BDBM225230
Substrate
n/a
Meas. Tech.
ChEMBL_2249039 (CHEMBL5163249)
IC50
15000±n/a nM
Citation
 Huang, Y; Sendzik, M; Zhang, J; Gao, Z; Sun, Y; Wang, L; Gu, J; Zhao, K; Yu, Z; Zhang, L; Zhang, Q; Blanz, J; Chen, Z; Dubost, V; Fang, D; Feng, L; Fu, X; Kiffe, M; Li, L; Luo, F; Luo, X; Mi, Y; Mistry, P; Pearson, D; Piaia, A; Scheufler, C; Terranova, R; Weiss, A; Zeng, J; Zhang, H; Zhang, J; Zhao, M; Dillon, MP; Jeay, S; Qi, W; Moggs, J; Pissot-Soldermann, C; Li, E; Atadja, P; Lingel, A; Oyang, C Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies. J Med Chem 65:5317-5333 (2022) [PubMed] 
Target
Name:
Alpha-2A adrenergic receptor
Synonyms:
ADA2A_HUMAN | ADRA2A | ADRA2R | ADRAR | Adrenergic alpha2A | Adrenergic receptor alpha | Alpha-2 adrenergic receptor subtype C10 | Alpha-2A adrenoceptor | Alpha-2A adrenoreceptor | Alpha-2AAR | alpha-2A adrenergic receptor [Homo sapiens]
Type:
Enzyme
Mol. Mass.:
48979.91
Organism:
Human
Description:
P08913
Residue:
465
Sequence:
MFRQEQPLAEGSFAPMGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFTSRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSSIVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGGPQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVAAPPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKASRWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSSLNPVIYTIFNHDFRRAFKKILCRGDRKRIV
  
Inhibitor
Name:
BDBM225230
Synonyms:
EED226 | US11013745, Compound EED226
Type:
Small organic molecule
Emp. Form.:
C17H15N5O3S
Mol. Mass.:
369.398
SMILES:
CS(=O)(=O)c1ccc(cc1)-c1cnc(NCc2ccco2)n2cnnc12
Structure:
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