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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 17 hits in this display   

TargetGTPase NRas(Homo sapiens (Human))
Massachusetts College Of Pharmacy And Health Sciences University

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataKi:  0.300nMAssay Description:Binding affinity to NRAS (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGTPase HRas(Homo sapiens (Human))
Massachusetts College Of Pharmacy And Health Sciences University

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataKi:  1.60nMAssay Description:Binding affinity to HRAS (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant FTase using [3H]farnesyldiphosphateMore data for this Ligand-Target Pair
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2nMAssay Description:Inhibitory concentration against farnesyltransferase was determinedMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2nMAssay Description:Inhibition of Farnesyl protein transferase radiolabel [1-3H] incorporationMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Bos taurus (bovine))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2nMAssay Description:Inhibition of Farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  3nMAssay Description:Concentration required to displace 50% of a radiolabelled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cellsMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  3.60nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Bos taurus (bovine))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  95nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells.More data for this Ligand-Target Pair
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  98nMAssay Description:Inhibition of human Geranylgeranyl transferase type I incorporation of [3H]-GGPP into biotinylated peptide corresponding to the C-terminus of human K...More data for this Ligand-Target Pair
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  98nMAssay Description:Inhibition of human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranylMore data for this Ligand-Target Pair
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  99nMAssay Description:Inhibition of geranyl-geranylation of the C-terminal CAAX sequence of Rap 1a in PSN-1 cellsMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2.00E+3nMAssay Description:In vitro inhibition against human Farnesyltransferase catalyzed by incorporation of [3H]- FPP into recombinant Ras-CVIMMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of [3H]-FPP incorporation into recombinant Ras-CVIM by human farnesyl transferaseMore data for this Ligand-Target Pair
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataIC50:  9.80E+4nMAssay Description:In vitro inhibition against human Geranylgeranyl transferase type I catalyzed by incorporation of [3H]- GGPP (geranylgeranyl pyrophosphate) into biot...More data for this Ligand-Target Pair
LigandPNGBDBM50097071(4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]MET...)
Affinity DataEC50:  6.80E+3nMAssay Description:Inhibition of Geranylgeranyl transferase type IMore data for this Ligand-Target Pair