Literature summary for 2.5.1.58 extracted from

Curtin, M.L.; Florjancic, A.S.; Cohen, J.; Gu, W.Z.; Frost, D.J.; Muchmore, S.W.; Sham, H.L.
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase (2003), Bioorg. Med. Chem. Lett., 13, 1367-1371.

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Inhibitors

Inhibitors	Comment	Organism	Structure
4-(3-{[(4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-methyl}-phenyl)-pyridine-2-carbonitrile	IC50: 0.37 nM, selective inhibitor	Rattus norvegicus
4-[(3'-Chloro-biphenyl-3-ylmethyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 0.45 nM, selective inhibitor	Rattus norvegicus
4-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 0.39 nM, selective inhibitor	Rattus norvegicus
4-[(3-Methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 31 nM	Rattus norvegicus
4-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 1.5 nM, selective inhibitor	Rattus norvegicus
4-[Biphenyl-3-ylmethyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 1.5 nM	Rattus norvegicus
4-[Hexyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 1.9 nM	Rattus norvegicus
4-[Methyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile	IC50: 38 nM	Rattus norvegicus
5-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile	IC50: 0.97 nM, selective inhibitor	Rattus norvegicus
5-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile	IC50: 10 nM, selective inhibitor	Rattus norvegicus
Biphenyl-3-carboxylic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide	IC50: 14 nM	Rattus norvegicus
Biphenyl-3-sulfonic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide	IC50: 18 nM	Rattus norvegicus
R115777	IC50: 0.57 nM, selective inhibitor	Rattus norvegicus
SCH66336	IC50: 7.8 nM, selective inhibitor	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00000037	-	IC50: 0.37 nM, selective inhibitor	Rattus norvegicus	4-(3-{[(4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-methyl}-phenyl)-pyridine-2-carbonitrile
0.00000045	-	IC50: 0.45 nM, selective inhibitor	Rattus norvegicus	4-[(3'-Chloro-biphenyl-3-ylmethyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
0.00000057	-	IC50: 0.57 nM, selective inhibitor	Rattus norvegicus	R115777
0.00000097	-	IC50: 0.97 nM, selective inhibitor	Rattus norvegicus	5-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile
0.0000015	-	IC50: 1.5 nM	Rattus norvegicus	4-[Biphenyl-3-ylmethyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
0.0000015	-	IC50: 1.5 nM, selective inhibitor	Rattus norvegicus	4-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
0.0000019	-	IC50: 1.9 nM	Rattus norvegicus	4-[Hexyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
0.0000078	-	IC50: 7.8 nM, selective inhibitor	Rattus norvegicus	SCH66336
0.00001	-	IC50: 10 nM, selective inhibitor	Rattus norvegicus	5-[(4-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2'-methyl-biphenyl-2-carbonitrile
0.000014	-	IC50: 14 nM	Rattus norvegicus	Biphenyl-3-carboxylic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide
0.000018	-	IC50: 18 nM	Rattus norvegicus	Biphenyl-3-sulfonic acid (4-cyano-3-naphthalen-1-yl-phenyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amide
0.000031	-	IC50: 31 nM	Rattus norvegicus	4-[(3-Methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
0.000038	-	IC50: 38 nM	Rattus norvegicus	4-[Methyl-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile
0.000039	-	IC50: 0.39 nM, selective inhibitor	Rattus norvegicus	4-[(3-cyano-benzyl)-(3-methyl-3H-imidazol-4-ylmethyl)-amino]-2-naphthalen-1-yl-benzonitrile

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Release 2023.1 (January 2023)