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Target
Muscarinic acetylcholine receptor M2
Ligand
BDBM50423967
Substrate
n/a
Meas. Tech.
ChEMBL_935578 (CHEMBL2320114)
EC50
>30000±n/a nM
Citation
 Le, U; Melancon, BJ; Bridges, TM; Vinson, PN; Utley, TJ; Lamsal, A; Rodriguez, AL; Venable, D; Sheffler, DJ; Jones, CK; Blobaum, AL; Wood, MR; Daniels, JS; Conn, PJ; Niswender, CM; Lindsley, CW; Hopkins, CR Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett 23:346-50 (2012) [PubMed]  Article
Target
Name:
Muscarinic acetylcholine receptor M2
Synonyms:
ACM2_HUMAN | CHRM2 | Cholinergic, muscarinic M2 | Muscarinic acetylcholine receptor M2 and M4 | Muscarinic acetylcholine receptor M2 and M5 | RecName: Full=Muscarinic acetylcholine receptor M2
Type:
GPCR
Mol. Mass.:
51730.61
Organism:
Homo sapiens (Human)
Description:
P08172
Residue:
466
Sequence:
MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNYFLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQFFSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRIVKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDEITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNIVARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNTVWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
  
Inhibitor
Name:
BDBM50423967
Synonyms:
CHEMBL2057417
Type:
Small organic molecule
Emp. Form.:
C16H15ClN4OS
Mol. Mass.:
346.835
SMILES:
Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl
Structure:
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