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Literature summary for 2.1.1.100 extracted from

  • Judd, W.R.; Slattum, P.M.; Hoang, K.C.; Bhoite, L.; Valppu, L.; Alberts, G.; Brown, B.; Roth, B.; Ostanin, K.; Huang, L.; Wettstein, D.; Richards, B.; Willardsen, J.A.
    Discovery and SAR of methylated tetrahydropyranyl derivatives as inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT) (2011), J. Med. Chem., 54, 5031-5047.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3,5-difluoro-4-methoxyphenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
Homo sapiens
(3-chloro-4-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
Homo sapiens
(3-chlorophenyl)-[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)ethyl]amine
-
Homo sapiens
(4-chloro-3-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
Homo sapiens
(5-chloro-2-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
Homo sapiens
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-fluorophenyl)thiourea
-
Homo sapiens
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxphenyl)urea
-
Homo sapiens
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxyphenyl)thiourea
-
Homo sapiens
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-phenylthiourea
-
Homo sapiens
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)thiourea
-
Homo sapiens
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)urea
-
Homo sapiens
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-(3-methoxyphenyl)acetamide
-
Homo sapiens
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-phenylacetamide
-
Homo sapiens
2-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl](phenyl)amino]-1-(furan-2-yl)ethanone
-
Homo sapiens
3,4-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2Hpyran-4-yl)ethyl]aniline
-
Homo sapiens
3,5-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
Homo sapiens
3-chloro-4-methyl-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)ethyl]aniline
-
Homo sapiens
3-chloro-4-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
-
Homo sapiens
3-chloro-N-(3-chlorophenyl)-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
-
Homo sapiens
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
Homo sapiens
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
Homo sapiens
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-methylaniline
-
Homo sapiens
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
Homo sapiens
3-chloro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
Homo sapiens
3-fluoro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
Homo sapiens
3-fluoro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
Homo sapiens
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
Homo sapiens
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
-
Homo sapiens
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
Homo sapiens
3-methoxy-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
Homo sapiens
3-methoxy-N-[2-[4-(4-methoxyphenyl)-2,2-dimethyltetrahydro-2H-pyran-4-yl]ethyl]aniline
-
Homo sapiens
3-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
Homo sapiens
3-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
Homo sapiens
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]benzoic acid
-
Homo sapiens
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]phenol
-
Homo sapiens
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]-N,N-dimethylbenzenesulfonamide
-
Homo sapiens
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
-
Homo sapiens
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-methylaniline
-
Homo sapiens
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
Homo sapiens
4-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
Homo sapiens
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzenesulfonamide
-
Homo sapiens
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
-
Homo sapiens
cysmethynil relatively potent in vitro inhibitor Homo sapiens
ethyl 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]amino]benzoate
-
Homo sapiens
FTI-2628
-
Homo sapiens
N'-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,N-dimethylbenzene-1,3-diamine
-
Homo sapiens
N-(3-chlorophenyl)-2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)acetamide
-
Homo sapiens
N-(3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]phenyl)acetamide
-
Homo sapiens
N-benzyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]furan-2-carboxamide
-
Homo sapiens
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)-ethyl]aniline
-
Homo sapiens
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-2-methylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,4-dimethoxyaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,5-dimethylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethoxy)aniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethyl)aniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-ethylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-fluoroaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-isopropylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxy-4-methylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxyaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-(trifluoromethoxy)aniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-fluoroaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-isopropylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methoxyaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,3-dimethylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-methylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-phenylacetamide
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3,4-dimethylaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-nitroaniline
-
Homo sapiens
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-nitroaniline
-
Homo sapiens
N-[3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-3-(2-methoxyphenyl)propyl]-N-(4-methoxybenzyl)furan-2-carboxamide the inhibitor is competitive with respect to a prenylated methyl acceptor substrate but noncompetitive toward the S-adenosyl-L-methionine Homo sapiens
[2-(2,2-dimethyl-4-p-tolyltetrahydropyran-4-yl)ethyl]-(3-methoxyphenyl)amine
-
Homo sapiens
[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-(2-fluorophenyl)amine
-
Homo sapiens
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(2-fluoro-4-methylphenyl)amine
-
Homo sapiens
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(3-fluoro-4-methoxyphenyl)amine
-
Homo sapiens
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]-(3-methoxyphenyl)amine
-
Homo sapiens
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]phenylamine
-
Homo sapiens
[2-[4-(3-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
Homo sapiens
[2-[4-(3-fluoro-phenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
Homo sapiens
[2-[4-(4-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
Homo sapiens
[2-[4-(4-fluorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
-
Homo sapiens
-
PC-3 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
-
Homo sapiens S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
-
?

Synonyms

Synonyms Comment Organism
Icmt
-
Homo sapiens
isoprenylcysteine carboxyl methyltransferase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000013
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
0.0000038
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens (3-chlorophenyl)-[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)ethyl]amine
0.000008
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-[4-(3-fluoro-phenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
0.000015
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxyaniline
0.000015
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)-ethyl]aniline
0.000019
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]-(3-methoxyphenyl)amine
0.000025
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
0.000025
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens (3-chloro-4-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
0.000026
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-nitroaniline
0.000031
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methylaniline
0.000031
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methylaniline
0.000031
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens (3,5-difluoro-4-methoxyphenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
0.000032
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens (5-chloro-2-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
0.00004
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-ethylaniline
0.000049
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-methylaniline
0.000052
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-fluoroaniline
0.000054
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,5-dimethylaniline
0.000066
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
0.000069
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3,4-dimethylaniline
0.00009
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxy-4-methylaniline
0.00009
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethoxy)aniline
0.0001
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-[4-(4-fluorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
0.00012
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-benzyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]furan-2-carboxamide
0.000123
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
0.000131
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N'-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,N-dimethylbenzene-1,3-diamine
0.000132
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-isopropylaniline
0.00016
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(3-fluoro-4-methoxyphenyl)amine
0.000167
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-isopropylaniline
0.000168
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-fluoroaniline
0.00017
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3,5-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
0.000181
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3,4-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2Hpyran-4-yl)ethyl]aniline
0.000184
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-(trifluoromethoxy)aniline
0.00019
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-[4-(3-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
0.00027
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methoxyaniline
0.00027
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]phenylamine
0.0003
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(2-fluoro-4-methylphenyl)amine
0.000308
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-methylaniline
0.00031
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 2-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl](phenyl)amino]-1-(furan-2-yl)ethanone
0.00036
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
0.00038
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethyl)aniline
0.00042
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
0.00046
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-4-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
0.00047
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens (4-chloro-3-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
0.00055
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-(2-fluorophenyl)amine
0.000556
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
0.00063
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-[4-(4-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
0.000652
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,4-dimethoxyaniline
0.000682
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-nitroaniline
0.00076
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 4-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
0.000777
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-methoxy-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-fluoro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-4-methyl-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)ethyl]aniline
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxphenyl)urea
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-phenylthiourea
0.001
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-fluorophenyl)thiourea
0.00135
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-(3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]phenyl)acetamide
0.00234
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-phenylacetamide
0.00249
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
0.0027
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
0.00288
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens ethyl 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]amino]benzoate
0.00325
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
0.00325
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-fluoro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
0.0035
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-3-(2-methoxyphenyl)propyl]-N-(4-methoxybenzyl)furan-2-carboxamide
0.0036
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-2-methylaniline
0.00383
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]-N,N-dimethylbenzenesulfonamide
0.00383
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
0.00419
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens [2-(2,2-dimethyl-4-p-tolyltetrahydropyran-4-yl)ethyl]-(3-methoxyphenyl)amine
0.005
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]phenol
0.005
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]benzoic acid
0.005
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-chloro-N-(3-chlorophenyl)-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
0.005
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-phenylacetamide
0.005
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-(3-methoxyphenyl)acetamide
0.005
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-(3-chlorophenyl)-2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)acetamide
0.00985
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,3-dimethylaniline
0.01
-
IC50 above 0.01 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-methylaniline
0.0125
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 3-methoxy-N-[2-[4-(4-methoxyphenyl)-2,2-dimethyltetrahydro-2H-pyran-4-yl]ethyl]aniline
0.0131
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzenesulfonamide
1
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)urea
1
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxyphenyl)thiourea
1
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C Homo sapiens 1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)thiourea