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Target
Muscarinic acetylcholine receptor M1
Ligand
BDBM50240693
Substrate
n/a
Meas. Tech.
ChEMBL_2062561 (CHEMBL4717814)
EC50
3900±n/a nM
Citation
 Davoren, JE; Lee, CW; Garnsey, M; Brodney, MA; Cordes, J; Dlugolenski, K; Edgerton, JR; Harris, AR; Helal, CJ; Jenkinson, S; Kauffman, GW; Kenakin, TP; Lazzaro, JT; Lotarski, SM; Mao, Y; Nason, DM; Northcott, C; Nottebaum, L; O'Neil, SV; Pettersen, B; Popiolek, M; Reinhart, V; Salomon-Ferrer, R; Steyn, SJ; Webb, D; Zhang, L; Grimwood, S Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects. J Med Chem 59:6313-28 (2016) [PubMed]  Article 
Target
Name:
Muscarinic acetylcholine receptor M1
Synonyms:
ACM1_HUMAN | CHRM1 | Cholinergic receptor, muscarinic 1 | Cholinergic, muscarinic M1
Type:
Protein
Mol. Mass.:
51442.54
Organism:
Homo sapiens (Human)
Description:
P11229
Residue:
460
Sequence:
MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVNNYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLISFDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYIQFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSSSERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEVVIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKEKKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYALCNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
  
Inhibitor
Name:
BDBM50240693
Synonyms:
CHEMBL4097569
Type:
Small organic molecule
Emp. Form.:
C22H23N3O3S
Mol. Mass.:
409.501
SMILES:
Cc1cnc(cc1Cc1ccc(cc1)-c1cscn1)C(=O)N[C@H]1CCOC[C@@H]1O |r|
Structure:
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