Reaction Details
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Muscarinic acetylcholine receptor M4
Ligand
BDBM48043
Substrate
n/a
Meas. Tech.
Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM): NMS Competition at rM4
EC50
87.1±n/a nM
Comments
modified from 0.0000871 20220104
Citation
PubChem, PC Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM): NMS Competition at rM4 PubChem Bioassay (2009)[AID] More Info.:
Target
Name:
Muscarinic acetylcholine receptor M4
Synonyms:
ACM4_RAT | Cholinergic, muscarinic M4 | Chrm-4 | Chrm4
Type:
Enzyme Catalytic Domain
Mol. Mass.:
52841.70
Organism:
RAT
Description:
Cholinergic, muscarinic M4 CHRM4 RAT::P08485
Residue:
477
Sequence:
MNFTPVNGSSANQSVRLVTAAHNHLETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQLQTVNNYFLFSLGCADLIIGAFSMNLYTLYIIKGYWPLGAVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTLAFLKSPLMKPSIKKPPPGGASREELRNGKLEEAPPPALPPPPRPVPDKDTSNESSSGSATQNTKERPPTELSTAEATTPALPAPTLQPRTLNPASKWSKIQIVTKQTGNECVTAIEIVPATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLVNTFCQSCIPERVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
Inhibitor
Name:
BDBM48043
Synonyms:
3-amino-4,6-dimethyl-N-p-anisyl-thieno[2,3-b]pyridine-2-carboxamide | 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-2-thieno[2,3-b]pyridinecarboxamide | 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide | 3-azanyl-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide | ML108 | VU0152100-1 | cid_864492
Type:
Small organic molecule
Emp. Form.:
C18H19N3O2S
Mol. Mass.:
341.427
SMILES:
COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1
Structure:
