Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T79961 | Target Info | |||
Target Name | Muscarinic acetylcholine receptor M5 (CHRM5) | ||||
Synonyms |
CHRM5
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Target Type | Successful Target | ||||
Gene Name | CHRM5 | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Poor Binders of This Target (in total, 97 binders) | Download | Top | |||
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Compound Name |
Carbachol
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Approved | Compound Info | ||
Synonyms |
Carbach; Carbacholin; Carbacholine; Carbacholinum; Carbacholum; Carbacol; Carbacolina; Carbacolo; Carbamiotin; Carbamoylcholine; Carbastat; Carbochol; Carbocholin; Carbocholine; Carbyl; Carcholin; Coletyl; Doryl; Jestryl; Karbachol; Lentin; Lentine; Miostat; Moryl; Rilentol; Vasoperif; CARBACHOL CHLORIDE; Carbachol hydrochloride; Carbacholine chloride; Carbacholini chloridum; Carbacholinium chloratum; Carbacholum chloratum; Carbacolo [DCIT]; Carbaminocholine chloride; Carbaminoylcholine chloride; Carbamoylcholine chloride; Carbamylcholine chloride; Choline carbamate chloride; Choline chloride carbamate; Choline chlorine carbamate; Isopto Carbachol; Karbachol [Czech]; Karbamoylcholin chlorid; Karbamoylcholin chlorid [Czech]; Lentine [French]; Mistura C; C 4382; TL 457; C-1770; Carbacholum [INN-Latin]; Carbacol [INN-Spanish]; Carbamic acid, ester with choline chloride; Carbamoylcholine-hydrochloride; Carbastat (TN); Carboptic (TN); Choline chloride, carbamate; Doryl (VAN); Doryl (pharmaceutical); Gamma-Carbamoyl choline chloride; Isopto Carbachol (TN); Miostat (TN); Carbachol [INN:BAN:JAN]; Choline, chloride carbamate(ester); Choline, chloride, carbamate; P. V. Carbachol; Carbachol (JAN/USP/INN); Choline, chloride, carbamate, hydrochloride; Ethanaminium, 2-(aminocarbonyl)oxy-N,N,N-trimethyl-, chloride; Ethanaminium, 2-[(aminocarbonyl)oxy]-N,N,N-trimethyl-, chloride; Ethanaminium, 2-((aminocarbonyl)oxy)-N,N,N-trimethyl-, chloride; Ethanaminium, 2-((aminocarbonyl)oxy)-N,N,N-trimethyl-, chloride (1:1); (2-Carbamoyloxy-ethyl)-trimethyl-ammonium; (2-Carbamoyloxy-ethyl)-trimethyl-ammonium(Carbachol); (2-Carbamoyloxyethyl)trimethylammonium chloride; (2-Hydroxyethyl)trimethyl ammonium chloride carbamate; (2-Hydroxyethyl)trimethylammonium chloride carbamate; (carbachol)(2-Carbamoyloxy-ethyl)-trimethyl-ammonium; 2-((Aminocarbonyl)oxy)-N,N,N-trimethylethanaminium chloride; 2-((Aminocarbonyl)oxy)-N,N,N-trimethylethanaminum chloride; 2-(carbamoyloxy)-N,N,N-trimethylethanaminium chloride; 2-[(aminocarbonyl)oxy]-N,N,N-trimethylethanaminium chloride; 2-carbamoyloxyethyl(trimethyl)azanium chloride
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Activity |
Ki = 69183.1 nM
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[1] | |||
Compound Name |
Arecoline
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Phase 1 | Compound Info | ||
Synonyms |
arecoline; Arecholine; Arecaline; 63-75-2; Methylarecaiden; Methylarecaidin; Arecolin; Arekolin; Arecoline base; Arecaidine methyl ester; Arecholin; methyl 1-methyl-1,2,5,6-tetrahydropyridine-3-carboxylate; 3-Pyridinecarboxylic acid, 1,2,5,6-tetrahydro-1-methyl-, methyl ester; Methyl N-methyltetrahydronicotinate; C8H13NO2; N-Methyltetrahydronicotinic acid, methyl ester; Methyl 1,2,5,6-tetrahydro-1-methylnicotinate; UNII-4ALN5933BH; NSC 56321; Methyl N-methyl-1,2,5,6-tetrahydronicotinate; CCRIS 7688
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Activity |
Ki = 56000 nM
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[2] | |||
Compound Name |
6-Fluoro-3-[1-[1-[[2-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL489576; BDBM50263936
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
2-[[4-[4-(2-Oxo-3H-benzimidazol-1-yl)piperidin-1-yl]piperidin-1-yl]methyl]benzonitrile
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Investigative | Compound Info | ||
Synonyms |
CHEMBL476990; BDBM50263413; 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-[1,4'']bipiperidinyl-1''-ylmethyl]-benzonitrile
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
6-Chloro-3-[1-[1-[[2-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL518747; BDBM50263371
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
3-[1-(1-Benzylpiperidin-4-yl)piperidin-4-yl]-6-chloro-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL490597; BDBM50263889; 1-(1''-Benzyl-[1,4'']bipiperidinyl-4-yl)-5-chloro-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
7-Fluoro-3-[1-[1-[(2-methylphenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL490598; BDBM50263890; 4-Fluoro-1-[1''-(2-methyl-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
7-Fluoro-3-[1-[1-[[2-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL521914; BDBM50263893
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
3-[1-[1-[(2-Chlorophenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL477821; SCHEMBL5476466; BDBM50263372; 1-[1''-(2-Chloro-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
3-[1-[1-[(2-Nitrophenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL478034; BDBM50263411; 1-[1''-(2-Nitro-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
6-Chloro-3-[1-[1-[(2-methylphenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL523657; BDBM50263837; 5-Chloro-1-[1''-(2-methyl-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
5-Fluoro-3-[1-[1-[[2-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL491818; BDBM50263937
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
2-[[4-[4-(5-Chloro-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]piperidin-1-yl]methyl]benzonitrile
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Investigative | Compound Info | ||
Synonyms |
CHEMBL491208; BDBM50263886; 2-[4-(5-Chloro-2-oxo-2,3-dihydro-benzoimidazol-1-yl)-[1,4'']bipiperidinyl-1''-ylmethyl]-benzonitrile
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
5-Fluoro-3-[1-[1-[(2-methylphenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL490797; BDBM50263892; 6-Fluoro-1-[1''-(2-methyl-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
6-Chloro-3-[1-[1-[(2-chlorophenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL515489; BDBM50263410; 5-Chloro-1-[1''-(2-chloro-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
6-Fluoro-3-[1-[1-[(2-methylphenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL522451; BDBM50263891; 5-Fluoro-1-[1''-(2-methyl-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
Tbpb
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Investigative | Compound Info | ||
Synonyms |
1-(1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one; CHEMBL522460; GTPL3258; SCHEMBL5473311; BCP13406; TBPB, >=98% (HPLC); BDBM50263887; ZINC40423557; AKOS026750197; CS-3517; NCGC00390669-01; DA-41854; HY-14562; QC-11734; FT-0746315; Y6339; A14205; BRD-K86989957-001-01-7; Q27088942; 1-(1''-(2-methylbenzyl)-1,4''-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one; 1-(1''-2-methylbenzyl)-1,4''-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one; 1-(1'-(2-Methylbenzyl)-[1,4'-bipiperidin]-4-yl)-1H-benzo[d]imidazol-2(3H)-one; 1-(1a?(2-Methylbenzyl)-1,4a?bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one
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Activity |
EC50 ~ 50000 nM
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[4] | |||
Compound Name |
3-[1-[1-[[2-(Trifluoromethyl)phenyl]methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL478662; SCHEMBL5486679; BDBM50263370; 1-(1''-(2-(trifluoromethyl)benzyl)-1,4''-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one; 1-[1''-(2-Trifluoromethyl-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
6-Chloro-3-[1-[1-[(2-nitrophenyl)methyl]piperidin-4-yl]piperidin-4-yl]-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL514689; BDBM50263412; 5-Chloro-1-[1''-(2-nitro-benzyl)-[1,4'']bipiperidinyl-4-yl]-1,3-dihydro-benzoimidazol-2-one
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Activity |
EC50 ~ 50000 nM
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[3] | |||
Compound Name |
(2R)-1,1-Dimethyl-2-[(2S,4R)-2-methyl-1,3-dioxolan-4-yl]pyrrolidin-1-ium
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Investigative | Compound Info | ||
Synonyms |
CHEMBL259131; BDBM50478147
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Activity |
Ki = 52480.75 nM
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[5] | |||
Compound Name |
N-[2-(Dimethylamino)ethyl]-N-methyl-1-(2-pyridinylmethylene)-1H-indene-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL279225; BDBM50219350
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Activity |
Ki = 52480.75 nM
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[6] | |||
Compound Name |
Trimethyl-[[(2R,6S)-5,5,6-trimethyl-1,4-dioxan-2-yl]methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL594803
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Activity |
Ki = 52480.75 nM
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[7] | |||
Compound Name |
N-[2-(Dimethylamino)ethyl]-N-methyl-1-(3-pyridinylmethylene)-1H-indene-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL21328; BDBM50219349
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Activity |
Ki = 53703.18 nM
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[6] | |||
Compound Name |
N-[2-(Dimethylamino)ethyl]-1-(4-pyridinylmethylene)-1H-indene-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL283320; BDBM50219351
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Activity |
Ki = 53703.18 nM
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[6] | |||
Compound Name |
N-[2-(Dimethylamino)ethyl]-1-(2-pyridinylmethylene)-1H-indene-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL21937; BDBM50219353
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Activity |
Ki = 54954.09 nM
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[6] | |||
Compound Name |
(4-Methylpiperazin-1-yl)-[(3E)-3-(pyridin-4-ylmethylidene)inden-1-yl]methanone
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Investigative | Compound Info | ||
Synonyms |
CHEMBL424214; BDBM50219397
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Activity |
Ki = 54954.09 nM
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[6] | |||
Compound Name |
(2S,3R,5S)-5-[(2S)-1,1-Dimethylpyrrolidin-1-ium-2-yl]-2-methyl-1,3-oxathiolane 3-oxide;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2093082; BDBM50475679
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Activity |
Ki = 57543.99 nM
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[8] | |||
Compound Name |
(2R,5R)-5-[(2S)-1,1-Dimethylpyrrolidin-1-ium-2-yl]-2-methyl-1,3-oxathiolane 3-oxide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL541424; BDBM50478149
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Activity |
Ki = 57543.99 nM
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[5] | |||
Compound Name |
N-Isopropyl-1-piperazineacetamide
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Investigative | Compound Info | ||
Synonyms |
n-isopropyl-2-(piperazin-1-yl)acetamide; N-isopropyl-2-piperazin-1-ylacetamide; 2-piperazin-1-yl-N-propan-2-ylacetamide; 2-(piperazin-1-yl)-N-(propan-2-yl)acetamide; CHEMBL2391356; 1-Piperazineacetamide, N-(1-methylethyl)-; N-(methylethyl)-2-piperazinylacetamide; EINECS 254-676-9; NSC379438; SCHEMBL255190; CTK4I2048; KS-00003TBM; DTXSID10192925; N-isopropyl-2-piperazinoacetamide; 2-piperazinyl-N-isopropylacetamide; N-isopropyl-1-piperazine acetamide; piperazinoacetic acid isopropylamide; ALBB-006203; 2503AE; BDBM50435342; MFCD00005969; SBB027314; STK501255; ZINC19942920; AKOS000264275; MCULE-4117297184; NSC-379438; VP70271; N-Isopropyl-1-piperazineacetamide, 95%; TS-02582; 1-Piperazineacetamide,N-(1-methylethyl)-; N-Isopropyl-2-(1-piperazinyl)acetamide #; DB-049493; BB 0259628; FT-0639584; ST45024241; EN300-18601; W-6183
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Activity |
IC50 = 63000 nM
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[9] | |||
Compound Name |
Pyrrolidine, 2-(2-furanyl)-1-methyl-, (2S)-
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Investigative | Compound Info | ||
Synonyms |
CHEMBL450729; BDBM50412424; ZINC40835745
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Activity |
Ki = 63095.73 nM
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[10] | |||
Compound Name |
Trimethyl-[[(2R,5S)-5-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL593443
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Activity |
Ki = 63095.73 nM
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[7] | |||
Compound Name |
N-[2-(Dimethylamino)ethyl]-3-(pyridin-3-ylmethyl)-1H-indene-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL355851; BDBM50474512
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Activity |
Ki = 66069.34 nM
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[11] | |||
Compound Name |
Trimethyl-[[(2R)-5,5,6,6-tetramethyl-1,4-dioxan-2-yl]methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL593861
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Activity |
Ki = 66069.34 nM
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[7] | |||
Compound Name |
N-[2-(Dimethylamino)ethyl]-1-(3-pyridinylmethylene)-1H-indene-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL279520; BDBM50219352
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Activity |
Ki = 66069.34 nM
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[6] | |||
Compound Name |
Trimethyl-[(6-methyl-1,4-dioxan-2-yl)methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL228144; BDBM50003014
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Activity |
Ki = 67608.3 nM
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[12] | |||
Compound Name |
Trimethyl-[[(2R,6R)-6-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL404557
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Activity |
Ki = 67608.3 nM
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[7] | |||
Compound Name |
Esaprazole
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Investigative | Compound Info | ||
Synonyms |
N-Cyclohexyl-2-piperazin-1-yl-acetamide; Exaprazole; N-cyclohexyl-2-piperazin-1-ylacetamide; N-cyclohexyl-2-(piperazin-1-yl)acetamide; N-Cyclohexyl-1-piperazineacetamide; UNII-38QSU0IB5L; 1-Piperazineacetamide, N-cyclohexyl-; Hexaprazol; 38QSU0IB5L; 1-Piperazineacetamide,N-cyclohexyl-; MFCD00865680; hexaprazole; NCGC00160434-01; DSSTox_CID_26147; DSSTox_RID_81379; DSSTox_GSID_46147; Esaprazole [INN]; Esaprazola; Esaprazolum; Esaprazolum [INN-Latin]; Esaprazola [INN-Spanish]; BRN 0785765; Prazol; N-cyclohexyl-2-piperazin-1-ylacetamide dihydrochloride; 5-23-02-00264 (Beilstein Handbook Reference); MLS004754470; SCHEMBL931007; CHEMBL1983100; DTXSID0046147; CTK5C0914; ALBB-013043; Tox21_111808; 7294AE; BDBM50435343; ZINC19737386; AKOS000209735; Tox21_111808_1; MCULE-8782683340; NE28840; N-cyclohexyl-2-(1-piperazinyl)acetamide; NCGC00160434-02; AS-44244; SMR002529465; n-(cyclohexyl-2-piperazin-1-yl)-acetamide; FT-0678584; EN300-68725; AE-641/00334033; AE-641/30178021; SR-01000883686; SR-01000883686-1; 1-piperazineacetamide, N-cyclohexyl-, dihydrochloride; BRD-K92426617-001-01-4; Q27256807; Z234896745
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Activity |
IC50 = 71000 nM
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[9] | |||
Compound Name |
2-[(8Ar)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-N-cyclohexylacetamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2391352; BDBM50435314
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Activity |
IC50 = 74000 nM
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[9] | |||
Compound Name |
Pyrrolidine, 2-(2-furanyl)-1-methyl-, (2R)-
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Investigative | Compound Info | ||
Synonyms |
CHEMBL461502; BDBM50412425; ZINC40861610
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Activity |
Ki = 75857.76 nM
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[10] | |||
Compound Name |
Trimethyl-[[(2R,6R)-5,5,6-trimethyl-1,4-dioxan-2-yl]methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL595022
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Activity |
Ki = 83176.38 nM
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[7] | |||
Compound Name |
Trimethyl-[[(2R,5R)-5-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL594376
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Activity |
Ki = 93325.43 nM
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[7] | |||
Compound Name |
[(2R,5R,6S)-5,6-Dimethyl-1,4-dioxan-2-yl]methyl-trimethylazanium;iodide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL608985
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Activity |
Ki = 97723.72 nM
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[7] | |||
Compound Name |
N-Cyclohexyl-2-(4-propanoylpiperazin-1-yl)acetamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2391367; SCHEMBL975152; BDBM50435331; AKOS032990511
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Activity |
IC50 ~ 100000 nM
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[9] | |||
Compound Name |
N,N,N-Trimethyl-alpha-(2-oxooxazolidine-5beta-yl)methaneaminium
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2441756
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Activity |
Ki ~ 100000 nM
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[13] | |||
Compound Name |
6,7,8,9-Tetrahydro-[1,2,5]thiadiazolo[3,4-h]isoquinoline
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL15936; [1,2,5]Thiadiazolo[3,4-h]isoquinoline, 6,7,8,9-tetrahydro; SCHEMBL7810242; BDBM50062157; 6,7,8,9-Tetrahydro-2-thia-1,3,8-triaza-cyclopenta[a]naphthalene
Click to Show/Hide
|
||||
Activity |
IC50 = 100000 nM
|
[14] | |||
Compound Name |
Ethyl 1-[2-(4-methoxyphenyl)ethyl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311977; BDBM50426228
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
Trimethyl-[[(2R,3R)-3-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL3309717
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[1] | |||
Compound Name |
(4R)-4-[(2S)-1-Methylpyrrolidin-2-yl]-1,3-oxazolidin-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441760
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
N-Pentan-3-yl-2-(4-propanoylpiperazin-1-yl)acetamide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2391366; SCHEMBL974224; BDBM50435332
Click to Show/Hide
|
||||
Activity |
IC50 ~ 100000 nM
|
[9] | |||
Compound Name |
[(2S)-1-(4-Methoxyphenyl)propan-2-yl] 1-ethyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312390; BDBM50426273
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(4-Methoxyphenyl)ethyl 1-[(4-methoxyphenyl)methyl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312385; BDBM50426257
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
(5S)-5-[(Dimethylamino)methyl]-3-methyl-1,3-oxazolidin-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441750
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
N,N,N-Trimethyl-alpha-(2-oxooxazolidine-5alpha-yl)methaneaminium
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441757
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
Trimethyl-[[(5S)-3-methyl-2-oxo-1,3-oxazolidin-5-yl]methyl]azanium
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441752
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl 1-butyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312363; BDBM50426251
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(3,4,5-Trimethoxyphenyl)ethyl 1-ethyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312380; BDBM50426262
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
(5R)-5-[(Dimethylamino)methyl]-3-methyl-1,3-oxazolidin-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441751
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
(5S,2''S)-5-(1-Methyl-2-pyrrolidinyl)oxazolidinone
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL500313; BDBM50256181
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
Trimethyl-[[(2R)-2-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL3309715
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[1] | |||
Compound Name |
[(2R,5S,6R)-5,6-Dimethyl-1,4-dioxan-2-yl]methyl-trimethylazanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL593864
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[7] | |||
Compound Name |
2-(3,4-Dimethoxyphenyl)ethyl 4-(3-methoxyphenyl)-1-methyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312356; BDBM50426231
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
(S)-5beta-[(Dimethylamino)methyl]oxazolidine-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441754; SCHEMBL21541688; (5S)-5-[(dimethylamino)methyl]-1,3-oxazolidin-2-one
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
2,3-Dihydro-1-benzofuran-5-ylmethyl 1-methyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312365; BDBM50426249
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
[(2S)-1-Methylpyrrolidin-2-yl]methyl carbamate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441758
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
1,4-Dimethyl-3-(4-methylthio-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydropyridine
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL279105; BDBM50062158; 1,4-Dimethyl-5-(4-methylsulfanyl-[1,2,5]thiadiazol-3-yl)-1,2,3,6-tetrahydro-pyridine
Click to Show/Hide
|
||||
Activity |
IC50 = 100000 nM
|
[14] | |||
Compound Name |
2-(3,4-Dimethoxyphenyl)ethyl 4-(2-fluorophenyl)-1-methyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312355; BDBM50426232
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
Ethyl 1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311978; BDBM50426227
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
[(2R,6R)-6-Ethyl-1,4-dioxan-2-yl]methyl-trimethylazanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2042401
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[16] | |||
Compound Name |
2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl 4-(3-fluorophenyl)-1-methyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312351; BDBM50426237
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
N-Cyclohexyl-2-(4-cyclopentylpiperazin-1-yl)-2-methylpropanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2391382; SCHEMBL974621; BDBM50435316
Click to Show/Hide
|
||||
Activity |
IC50 ~ 100000 nM
|
[9] | |||
Compound Name |
2-(2,4,6-Trimethylphenyl)ethyl 1-ethyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312381; BDBM50426261
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(3,4-Dimethoxyphenyl)ethyl 4-(2-methoxyphenyl)-1-methyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312357; BDBM50426230
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(4-Cyclohexylpiperazin-1-yl)-2-methyl-N-propan-2-ylpropanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2391374; BDBM50435324
Click to Show/Hide
|
||||
Activity |
IC50 ~ 100000 nM
|
[9] | |||
Compound Name |
Ethyl 1-[1-(2,6-dimethylbenzoyl)piperidin-4-yl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311980; BDBM50426225
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
Ethyl 1-[2-(1,3-benzodioxol-5-yl)ethyl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311979; BDBM50426226
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
Ethyl 1-[1-(4-methylphenyl)sulfonylpiperidin-4-yl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311982; BDBM50426223
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(4-Methoxyphenyl)ethyl 1-butyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312360; BDBM50426254
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl 2-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)benzoate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312345; BDBM50426279
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl 4-phenyl-1-propyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312362; BDBM50426252
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
(2-Methoxy-2-phenylethyl) 1-methyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312348; BDBM50426240
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
(5R,2''S)-5-(1-Methyl-2-pyrrolidinyl)oxazolidinone
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL220553; BDBM50194316; (5R,2''S)-5[1''-methylpyrrolidin-2''-yl]-1,3-oxazolidin-2-one
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
Trimethyl-[[(2R,3S)-3-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL3359597
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[1] | |||
Compound Name |
Trimethyl-[[(5R)-3-methyl-2-oxo-1,3-oxazolidin-5-yl]methyl]azanium
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441753
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
Ethyl 4-phenyl-1-(2-phenylethyl)-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311976; BDBM50426229
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
2-(4-Methoxyphenyl)ethyl 4-phenyl-1-propyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312359; BDBM50426255
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
[(2S)-1,1-Dimethylpyrrolidin-1-ium-2-yl]methyl carbamate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441759
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
[(2R)-5,5-Dimethyl-1,4-dioxan-2-yl]methyl-trimethylazanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL594802
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[7] | |||
Compound Name |
2-(4-Methylsulfonylphenyl)ethyl 1-ethyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2312375; BDBM50426267
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
N-Cyclohexyl-2-(4-cyclopentylpiperazin-1-yl)acetamide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2391368; SCHEMBL976125; BDBM50435329
Click to Show/Hide
|
||||
Activity |
IC50 ~ 100000 nM
|
[9] | |||
Compound Name |
N-Cyclohexyl-2-(4-methyl-1,4-diazepan-1-yl)acetamide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2391357; SCHEMBL1024404; BDBM50435341
Click to Show/Hide
|
||||
Activity |
IC50 ~ 100000 nM
|
[9] | |||
Compound Name |
(R)-5alpha-[(Dimethylamino)methyl]oxazolidine-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441755
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
Ethyl 1-[1-(2,6-dichlorobenzoyl)piperidin-4-yl]-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2311981; BDBM50426224
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[15] | |||
Compound Name |
(4S)-4-[(2S)-1-Methylpyrrolidin-2-yl]-1,3-oxazolidin-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL2441761
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[13] | |||
Compound Name |
[(2R,5R,6R)-5,6-Dimethyl-1,4-dioxan-2-yl]methyl-trimethylazanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL593871
Click to Show/Hide
|
||||
Activity |
Ki ~ 100000 nM
|
[7] | |||
Compound Name |
1,1-Diphenyl-4-(4-phenylpiperazin-1-yl)butan-1-ol;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL403029
Click to Show/Hide
|
||||
Activity |
Ki = 123026.88 nM
|
[17] | |||
Compound Name |
Pyrrolidine, 2-(5-methyl-2-furanyl)-, (2S)-
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL458416; ZINC4234800; BDBM50412426; AKOS006329069
Click to Show/Hide
|
||||
Activity |
Ki = 138038.43 nM
|
[10] | |||
Compound Name |
3-Methoxy-4-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazole;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL553058
Click to Show/Hide
|
||||
Activity |
EC50 = 199526.23 nM
|
[18] | |||
Click to Show/Hide the Information of All Poor Binders |
Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
---|---|---|---|---|---|
Compound Name |
4-[2-[(4-Hydroxy-4,4-diphenylbutyl)-methylamino]ethyl-methylamino]-1,1-diphenylbutan-1-ol;dihydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL255692
Click to Show/Hide
|
||||
Activity |
Ki = 229086.77 nM
|
[17] | |||
Compound Name |
Trimethyl-[[(2R,6S)-6-methyl-1,4-dioxan-2-yl]methyl]azanium;iodide
Click to Show/Hide
|
Investigative | Compound Info | ||
Synonyms |
CHEMBL390842
Click to Show/Hide
|
||||
Activity |
EC50 = 2.69E+14 nM
|
[19] |
References | Top | ||||
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REF 1 | Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3255-9. | ||||
REF 2 | C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists. J Med Chem. 2003 May 22;46(11):2216-26. | ||||
REF 3 | Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5439-42. | ||||
REF 4 | Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5443-7. | ||||
REF 5 | Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding. Bioorg Med Chem. 2008 Mar 15;16(6):3049-58. | ||||
REF 6 | Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands. Bioorg Med Chem Lett. 2001 May 7;11(9):1241-3. | ||||
REF 7 | Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation. Bioorg Med Chem. 2009 Dec 15;17(24):8174-85. | ||||
REF 8 | Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist. J Med Chem. 2006 Mar 23;49(6):1925-31. | ||||
REF 9 | Synthesis and biological evaluation of Esaprazole analogues showing 1 binding and neuroprotective properties in vitro. Bioorg Med Chem. 2013 Jun 1;21(11):3334-47. | ||||
REF 10 | Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists. J Med Chem. 2008 Jul 10;51(13):3905-12. | ||||
REF 11 | Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists. J Med Chem. 2003 Feb 27;46(5):856-67. | ||||
REF 12 | Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide. Bioorg Med Chem Lett. 2008 Jan 15;18(2):614-8. | ||||
REF 13 | Design, synthesis and binding affinity of acetylcholine carbamoyl analogues. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6481-5. | ||||
REF 14 | Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity. J Med Chem. 1998 Jan 1;41(1):109-16. | ||||
REF 15 | Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists. J Med Chem. 2013 Feb 28;56(4):1693-703. | ||||
REF 16 | 1,4-dioxane, a suitable scaffold for the development of novel M1 muscarinic receptor antagonists. J Med Chem. 2012 Feb 23;55(4):1783-7. | ||||
REF 17 | Diphenidol-related diamines as novel muscarinic M4 receptor antagonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2972-6. | ||||
REF 18 | Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders. J Med Chem. 2003 Sep 25;46(20):4273-86. | ||||
REF 19 | Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists. Bioorg Med Chem. 2007 Jan 15;15(2):886-96. |
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