Target
Muscarinic acetylcholine receptor M1
Ligand
BDBM50185431
Substrate
n/a
Meas. Tech.
ChEMBL_1588015 (CHEMBL3824950)
EC50
6166±n/a nM
Citation
 Panarese, JDCho, HPAdams, JJNance, KDGarcia-Barrantes, PMChang, SMorrison, RDBlobaum, ALNiswender, CMStauffer, SRConn, PJLindsley, CW Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. Bioorg Med Chem Lett 26:3822-5 (2016) [PubMed]  Article 
Target
Name:
Muscarinic acetylcholine receptor M1
Synonyms:
ACM1_RAT | Cholinergic, muscarinic M1 | Chrm-1 | Chrm1 | cholinergic receptor, muscarinic 1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51390.46
Organism:
RAT
Description:
P08482
Residue:
460
Sequence:
MNTSVPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVNNYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLISFDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYIQFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSSSERSQPGAEGSPESPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEVVIKMPMVDSEAQAPTKQPPKSSPNTVKRPTKKGRDRGGKGQKPRGKEQLAKRKTFSLVKEKKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTVNPMCYALCNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
  
Inhibitor
Name:
BDBM50185431
Synonyms:
CHEMBL3823781
Type:
Small organic molecule
Emp. Form.:
C23H14F2N4O
Mol. Mass.:
400.3803
SMILES:
Fc1cc(cc(F)c1Cn1cnc2cnccc2c1=O)-c1ccc2cnccc2c1
Structure:
Search PDB for entries with ligand similarity: