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Found 301 with Last Name = 'heimbrook' and Initial = 'dc'
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50181139((S)-2-amino-2-cyclopropyl-1-((S)-4-(2,5-difluoroph...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM16179(4-{[5-({[(3S)-1-(3-chlorobenzyl)-2-oxopyrrolidin-3...)
Affinity DataIC50:  0.520nMAssay Description:Concentration required to displace 50% of a potent radiolabeled FTI from farnesyl transferase in cultured H-ras-transformed Rat1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012304(2-{2-[2-[2-(2,2-Dimethyl-propionylamino)-3-(3H-imi...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14018((17R, 20R)-19,20,21,22-Tetrahydro-19-oxo-17H-15,-1...)
Affinity DataIC50: <1nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14025((1R,2R,5R)-30-oxo-19,24-dioxa-2,6,10,12-tetraazahe...)
Affinity DataIC50: <1nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14023((1R,2R,5R)-30-oxo-19-oxa-2,6,10,12-tetraazahexacyc...)
Affinity DataIC50: <1nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14014((5S)-31-oxo-20-oxa-2,6,11,13-tetraazahexacyclo[19....)
Affinity DataIC50:  1.10nMAssay 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
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50103360((3-{[1-(3-Chloro-benzyl)-2-oxo-pyrrolidin-3-yl]-[3...)
Affinity DataIC50:  1.10nMAssay Description:Concentration required to displace 50% of a potent radiolabeled FTI from farnesyl transferase in cultured H-ras-transformed Rat1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14017((5R)-6-methyl-31-oxo-20-oxa-2,6,11,13-tetraazahexa...)
Affinity DataIC50:  1.20nMAssay 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 DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50181138((S)-2-amino-1-((S)-4-(2,5-difluorophenyl)-2-(3-hyd...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012313(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  1.20nMAssay Description:Compound was evaluated for mitogenic inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14015((5R)-31-oxo-20-oxa-2,6,11,13-tetraazahexacyclo[19....)
Affinity DataIC50:  1.20nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14008((11R)-32-oxo-25-oxa-8,12,16,18-tetraazahexacyclo[2...)
Affinity DataIC50:  1.30nMpH: 7.5 T: 2°CAssay 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 DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50103360((3-{[1-(3-Chloro-benzyl)-2-oxo-pyrrolidin-3-yl]-[3...)
Affinity DataIC50:  1.30nMAssay Description:In vitro inhibition of farnesyl transferase using purified recombinant human enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50181137((S)-1-((S)-4-(2,5-difluorophenyl)-2-(3-hydroxyphen...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14007((6R)-24-bromo-27-oxo-20-oxa-3,7,11,13-tetraazapent...)
Affinity DataIC50:  1.40nMpH: 7.5 T: 2°CAssay 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 DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012318(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14022((1R,2R,5R)-6-methyl-29-oxo-19-oxa-2,6,10,12-tetraa...)
Affinity DataIC50:  1.40nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14016((5S)-6-methyl-31-oxo-20-oxa-2,6,11,13-tetraazahexa...)
Affinity DataIC50:  1.5nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14024((1R,2R,5S)-30-oxo-19-oxa-2,6,10,12-tetraazahexacyc...)
Affinity DataIC50:  1.5nMAssay 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 DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50103333(4-(5-{[1-(2-Chloro-phenyl)-2-oxo-pyrrolidin-3-ylam...)
Affinity DataIC50:  1.5nMAssay Description:In vitro inhibition of farnesyl transferase using purified recombinant human enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14010((20R)-19,20,21,22-Tetrahydro-19-oxo-5H-18,20-ethan...)
Affinity DataIC50:  1.60nMpH: 7.5 T: 2°CAssay 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
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012306(Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 | CHEMBL274...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012304(2-{2-[2-[2-(2,2-Dimethyl-propionylamino)-3-(3H-imi...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14005((20R)-19,20,21,22-Tetrahydro-5-methyl-19-oxo-17H-1...)
Affinity DataIC50:  1.90nMpH: 7.5 T: 2°CAssay 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 DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM16179(4-{[5-({[(3S)-1-(3-chlorobenzyl)-2-oxopyrrolidin-3...)
Affinity DataIC50:  1.90nMAssay Description:In vitro inhibition of farnesyl transferase using purified recombinant human enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM5284(4-{[4-(Methylsulfonyl)piperazin-1-yl]methyl}-N-(5-...)
Affinity DataIC50:  2nMpH: 7.4 T: 2°CAssay Description:Activated KDR was incubated with 25 uM/10 uCi of [gamma-33P] ATP, poly-Glu/Tyr, and inhibitors in kinase buffer for 15 min at 22 °C. The reactio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012317(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  2nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM24060((2S)-2-amino-2-cyclopropyl-1-[(2S)-4-(2,5-difluoro...)
Affinity DataIC50:  2nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14012((5S)-7,31-dioxo-20-oxa-2,6,11,13-tetraazahexacyclo...)
Affinity DataIC50:  2.10nMpH: 7.5 T: 2°CAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14013((5R)-7,31-dioxo-20-oxa-2,6,11,13-tetraazahexacyclo...)
Affinity DataIC50:  2.30nMAssay 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 DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012311(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  2.40nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50103322(4-(5-{[[1-(3-Chloro-benzyl)-2-oxo-pyrrolidin-3-yl]...)
Affinity DataIC50:  2.5nMAssay Description:In vitro inhibition of farnesyl transferase using purified recombinant human enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14003((20R)-17-(3-Chlorophenyl)-19,20,21,22-tetrahydro-1...)
Affinity DataIC50:  2.5nMpH: 7.5 T: 2°CAssay 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 DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM24054((2S)-4-(2,5-difluorophenyl)-N-methyl-2-phenyl-N-(p...)
Affinity DataIC50:  2.60nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012307(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  2.60nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM24061((2S)-2-amino-1-[(2S)-4-(2,5-difluorophenyl)-2-phen...)
Affinity DataIC50:  2.70nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50103318(4-(5-{[1-(2-Chloro-benzyl)-2-oxo-pyrrolidin-3-ylam...)
Affinity DataIC50:  2.70nMAssay Description:Concentration required to displace 50% of a potent radiolabeled FTI from farnesyl transferase in cultured H-ras-transformed Rat1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012308(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50181141((S)-2-cyclopropyl-1-((S)-4-(2,5-difluorophenyl)-2-...)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012318(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  3nMAssay Description:Compound was evaluated for mitogenic inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM5282((5-Phenylthiazol-2-yl)(4-pyrrolidin-1-ylmethylpyri...)
Affinity DataIC50:  3nMpH: 7.4 T: 2°CAssay Description:Activated KDR was incubated with 25 uM/10 uCi of [gamma-33P] ATP, poly-Glu/Tyr, and inhibitors in kinase buffer for 15 min at 22 °C. The reactio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012309(Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2 | CHEMBL2...)
Affinity DataIC50:  3.20nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012297(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propio...)
Affinity DataIC50:  3.30nMAssay Description:Compound was evaluated for mitogenic inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Protein farnesyltransferase subunit beta(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50103334(4-(5-{[[1-(3-Chloro-benzyl)-2-oxo-pyrrolidin-3-yl]...)
Affinity DataIC50:  3.30nMAssay Description:Concentration required to displace 50% of a potent radiolabeled FTI from farnesyl transferase in cultured H-ras-transformed Rat1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM13998((20R)-19,20,21,22-Tetrahydro-19-oxo-17H-18,20-etha...)
Affinity DataIC50:  3.5nMpH: 7.5 T: 2°CAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14009((20S)-19,20,21,22-Tetrahydro-19-oxo-5H-18,20-ethan...)
Affinity DataIC50:  3.5nMpH: 7.5 T: 2°CAssay 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
LigandPNGBDBM14020((1R,2R,5S)-29-oxo-19-oxa-2,6,10,12-tetraazahexacyc...)
Affinity DataIC50:  3.60nMAssay 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 DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM24058((2S)-2-amino-1-[(2S)-4-(2,5-difluorophenyl)-2-phen...)
Affinity DataIC50:  3.60nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastrin-releasing peptide receptor(MOUSE)
Merck Sharp & Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012300(2-[2-[2-(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-y...)
Affinity DataIC50:  3.90nMAssay Description:Inhibition against Swiss 3T3 murine fibroblast cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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