Reaction Details
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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM48060
Substrate
n/a
Meas. Tech.
Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Analog Potency
EC50
8240±n/a nM
Citation
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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:
BDBM48060
Synonyms:
3-amino-4-methyl-N-p-anisyl-6-(2-pyrrolidinoethoxy)thieno[2,3-b]pyridine-2-carboxamide | 3-amino-N-[(4-methoxyphenyl)methyl]-4-methyl-6-(2-pyrrolidin-1-ylethoxy)thieno[2,3-b]pyridine-2-carboxamide | 3-amino-N-[(4-methoxyphenyl)methyl]-4-methyl-6-[2-(1-pyrrolidinyl)ethoxy]-2-thieno[2,3-b]pyridinecarboxamide | 3-azanyl-N-[(4-methoxyphenyl)methyl]-4-methyl-6-(2-pyrrolidin-1-ylethoxy)thieno[2,3-b]pyridine-2-carboxamide | VU0152120 | cid_45142472
Type:
Small organic molecule
Emp. Form.:
C23H28N4O3S
Mol. Mass.:
440.558
SMILES:
COc1ccc(CNC(=O)c2sc3nc(OCCN4CCCC4)cc(C)c3c2N)cc1