Compile Data Set for Download or QSAR
Report error Found 1001 Enz. Inhib. hit(s) with Target = 'Geranylgeranyl transferase type-1 subunit beta'
LigandPNGBDBM14434(Racemic mixture | R-115777 | 6-[amino(4-chlorophen...)
Affinity DatapH: 7.5 T: 2°CAssay Description:Compounds were tested as inhibitors of GGTase-1 in vitro using purified human enzyme to catalyze the reaction between [3H] GGPP and a biotinylated pe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/4/2007
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50112379(1-(3-Chloro-phenyl)-4-{2-[3-(2-methoxy-4'-trifluor...)
Affinity DataEC50:  3.40E+3nMAssay Description:Inhibition of geranylgeranylation of Rap1a in PSN-1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50112383(17-(5,5,5-trifluoropentyl)-19-oxa-2,5,10,12-tetraa...)
Affinity DataEC50:  800nMAssay Description:Inhibition of geranylgeranylation of Rap1a in PSN-1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50097071(4-{5-[4-(3-Chloro-phenyl)-3-oxo-piperazin-1-ylmeth...)
Affinity DataEC50:  6.80E+3nMAssay Description:Inhibition of Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50130374(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataEC50: >1.00E+3nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50130372(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataEC50:  87nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50130378(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataEC50:  220nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50130368(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataEC50:  3.99E+3nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50130373(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataEC50:  250nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50130365(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataEC50:  47nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50409707(CHEMBL2111612)
Affinity DataEC50:  720nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50409708(CHEMBL400694)
Affinity DataEC50:  3.20E+3nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50409709(CHEMBL439047)
Affinity DataEC50:  140nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50143599(4-[(S)-1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl...)
Affinity DataEC50:  470nMAssay Description:Inhibition of Rap1a protein geranylgeranylation in human PSN1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50115928(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataEC50:  50nMAssay Description:Inhibition of geranylgeranylation of the C-terminal CAAX sequence of Rap 1a in PSN-1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115911(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataEC50:  71nMAssay Description:Inhibition of geranylgeranylation of the C-terminal CAAX sequence of Rap 1a in PSN-1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115916(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataEC50:  18nMAssay Description:Inhibition of geranylgeranylation of the C-terminal CAAX sequence of Rap 1a in PSN-1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115923(4-[3-(4-Cyano-benzyl)-2-methyl-3H-imidazol-4-ylmet...)
Affinity DataEC50:  680nMAssay Description:Inhibition of geranylgeranylation of C-terminal CAAX sequence of Rap 1a in PSN-1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115916(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 0.160nMAssay Description:Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50098037(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 0.200nMAssay Description:Inhibitory activity against human Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/5/2012
Entry Details Article
PubMed
LigandPNGBDBM50115911(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 0.320nMAssay Description:Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115919(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 0.320nMAssay Description:Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115914(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50130374(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataIC50: 0.810nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50115925(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 0.840nMAssay Description:Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50059858((S)-2-((3Z,6E)-(2S,5S,8R)-8-Amino-2-benzyl-5-isopr...)
Affinity DataIC50: 1nMAssay Description:In vitro inhibitory activity against Geranylgeranyl transferase in the geranylgeranylation of H-ras-CAIL proteinMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50048966((R)-2-({(S)-2-[(S)-2-((R)-2-Amino-3-mercapto-propy...)
Affinity DataIC50: 1.30nMAssay Description:In vitro inhibition of Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM13382(CHEMBL158553 | 3-(3-chlorophenyl)-4-{[(4-cyanophen...)
Affinity DataIC50: 1.30nMAssay Description:inhibitory concentration needed to to reduce the bovine GGTase-catalyzed incorporation of [3H]-FPP into a biotin-linked K-ras (B) decapeptideMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50130373(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataIC50: 1.40nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50139187(4-(2-cyclohexylethyl)-23-oxo-8-oxa-1,15,17,21-tetr...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human Geranylgeranyl transferase type I incorporation of [3H]GGPP into biotinylated peptide corresponding to the C-terminus of human Ki...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50040692((S)-2-{(S)-2-[(S)-2-((R)-2-Amino-3-mercapto-propyl...)
Affinity DataIC50: 1.90nMAssay Description:Inhibitory activity against bovine type-1 geranylgeranyl transferase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/28/2012
Entry Details Article
PubMed
LigandPNGBDBM50139188(4-(3,3-dimethylbutyl)-23-oxo-8-oxa-1,15,17,21-tetr...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of human Geranylgeranyl transferase type I incorporation of [3H]GGPP into biotinylated peptide corresponding to the C-terminus of human Ki...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50130372(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataIC50: 2.10nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50139184(4-(2-cyclohexyl-1-ethynyl)-23-oxo-8-oxa-1,15,17,21...)
Affinity DataIC50: 2.40nMAssay Description:Inhibition of human Geranylgeranyl transferase type I incorporation of [3H]GGPP into biotinylated peptide corresponding to the C-terminus of human Ki...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50130365(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataIC50: 2.5nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50135353(5-(3-Chloro-phenyl)-6-[(4-cyano-phenyl)-(3-methyl-...)
Affinity DataIC50: 2.70nMAssay Description:inhibitory concentration needed to to reduce the bovine GGTase-catalyzed incorporation of [3H]-FPP into a biotin-linked K-ras (B) decapeptideMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50130378(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataIC50: 2.90nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
TargetGeranylgeranyl transferase type-1 subunit beta(Human)
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50126030(4-[1-Hydroxy-1-(3-methyl-3H-imidazol-4-yl)-3-pheny...)
Affinity DataIC50: 3.10nMAssay Description:Inhibition of human GGTase-catalyzed incorporation of [3H]GGPP into biotinylated peptide of C-terminal of human K-RasMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50143599(4-[(S)-1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl...)
Affinity DataIC50: 3.60nMAssay Description:Inhibition binding constant Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50143599(4-[(S)-1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl...)
Affinity DataIC50: 3.60nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50409707(CHEMBL2111612)
Affinity DataIC50: 4.5nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMed
LigandPNGBDBM50048963((R)-2-({(S)-2-[(S)-2-((R)-2-Amino-3-mercapto-propy...)
Affinity DataIC50: 4.80nMAssay Description:In vitro inhibition of Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50112372(17-(5,5,5-trifluoro-1-pentynyl)-19-oxa-2,5,10,12-t...)
Affinity DataIC50: 4.80nMAssay Description:Inhibition of the human Geranylgeranyl transferase type I catalyzed incorporation of [3H]GGPP into a biotinylated peptide corresponding to the C-term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50115928(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50: 4.80nMAssay Description:Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50128463((S)-2-{[1-((R)-2-Amino-3-mercapto-propionyl)-4-phe...)
Affinity DataIC50: 5nMAssay Description:Inhibition of Candida albicans Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50128465((S)-2-{[1-((R)-2-Amino-3-mercapto-propionyl)-4-phe...)
Affinity DataIC50: 5nMAssay Description:Inhibition of Candida albicans Geranylgeranyl transferase type IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50076128((S)-2-{[5-((R)-2-Amino-3-mercapto-propylamino)-bip...)
Affinity DataIC50: 5nMAssay Description:Inhibition of GGTase1 isolated from human Burkitt's lymphoma cells assessed as decrease in transfer of [3H]H]geranylgeranyl from [3H]geranylgeranyl P...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM50076128((S)-2-{[5-((R)-2-Amino-3-mercapto-propylamino)-bip...)
Affinity DataIC50: 5nMAssay Description:Inhibition of human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranylMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
LigandPNGBDBM50130367(4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-...)
Affinity DataIC50: 5.10nMAssay Description:Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14014(CHEMBL55826 | (5S)-31-oxo-20-oxa-2,6,11,13-tetraaz...)
Affinity DataIC50: 5.5nMAssay Description:Compounds were tested as inhibitors of FTase in vitro using purified recombinant human enzyme to catalyze the reaction between [3H]FPP and a recombin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2007
Entry Details Article
PubMed
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