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Found 587 with Last Name = 'abrams' and Initial = 't'
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50169743((13S,17S)-13-Methyl-7-[9-(4,4,5,5,5-pentafluoro-pe...)
Affinity DataIC50:  0.0600nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as inhibition of insulin-mediated cell proliferation after 6 days by Hoechst 33258 dye-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50101929(3-oxo-18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,...)
Affinity DataIC50:  0.100nMAssay Description:In vitro inhibitory activity to reduce the human farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139186(4-allyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacyclo...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50101929(3-oxo-18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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 DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM269467((E)-3-(4-((2-(2-(1,1- difluoroethyl)phenyl)-6- hyd...)
Affinity DataIC50:  0.200nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM269484(US10058534, 139)
Affinity DataIC50:  0.200nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysisMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139202(4-methyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacycl...)
Affinity DataIC50:  0.260nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50101929(3-oxo-18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,...)
Affinity DataIC50:  0.290nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139196(4-chloro-23-oxo-8-oxa-1,15,17,21-tetraazapentacycl...)
Affinity DataIC50:  0.300nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223460(6-(3-aminopropyl)-4-(4-hydroxyphenyl)-9-(1H-pyrazo...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM269456((E)-3-(4-((2-(2-(1- fluoroethyl)phenyl)-6- hydroxy...)
Affinity DataIC50:  0.300nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139190(4-propyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacycl...)
Affinity DataIC50:  0.310nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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 DepthDetails ArticlePubMed
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 DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139202(4-methyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacycl...)
Affinity DataIC50:  0.330nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50115927(4-[3-(4-Cyano-benzyl)-2-methyl-3H-imidazol-4-ylmet...)
Affinity DataIC50:  0.330nMAssay Description:Inhibition of Farnesyl protein transferase radiolabel [1-3H] incorporationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50115927(4-[3-(4-Cyano-benzyl)-2-methyl-3H-imidazol-4-ylmet...)
Affinity DataIC50:  0.340nMAssay Description:Displacement of radiolabeled farnesyl transferase inhibitorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50115916(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50:  0.360nMAssay Description:Inhibitor of Farnesyl protein transferase(FTPase) required to reduce radiolabel [1-3H] incorporation by 50%More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM269308((E)-3-(4-((6-hydroxy-2- (2-isopropylphenyl)- benzo...)
Affinity DataIC50:  0.400nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237322(CHEMBL4088736)
Affinity DataIC50:  0.400nMAssay Description:Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237304(CHEMBL4093325)
Affinity DataIC50:  0.400nMAssay Description:In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139190(4-propyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacycl...)
Affinity DataIC50:  0.440nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139189(4-bromo-23-oxo-8-oxa-1,15,17,21-tetraazapentacyclo...)
Affinity DataIC50:  0.450nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50101925(16-benzyl-17-oxo-(16R)-2-oxa-9,11,15,18-tetraazape...)
Affinity DataIC50:  0.470nMAssay Description:In vitro inhibitory activity to reduce the human farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139195(4-(2,2-dimethyl-1,3-dioxolan-4-ylmethyl)-23-oxo-8-...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223478(6-(2-aminoethyl)-9-(1H-pyrrol-2-yl)benzo[h]isoquin...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50090462(CHEMBL3581693)
Affinity DataIC50:  0.5nMAssay Description:Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237317(CHEMBL4098286)
Affinity DataIC50:  0.5nMAssay Description:Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139198(4-(1-ethynyl)-23-oxo-8-oxa-1,15,17,21-tetraazapent...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139186(4-allyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacyclo...)
Affinity DataIC50:  0.590nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237305(CHEMBL4072611)
Affinity DataIC50:  0.600nMAssay Description:Affinity of compound for Dopamine receptor D2 in rat striatal membrane determined for antagonist state (low affinity state, D2 Low) with [3H]spiperon...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103307(US8546434, 4)
Affinity DataIC50:  0.600nMpH: 7.5 T: 2°CAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237332(CHEMBL4078937)
Affinity DataIC50:  0.600nMAssay Description:Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223480(6-(2-aminoethyl)-9-(4-(morpholinomethyl)phenyl)ben...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139200(4-cyclopropylmethyl-23-oxo-8-oxa-1,15,17,21-tetraa...)
Affinity DataIC50:  0.660nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139191(4-ethyl-23-oxo-8-oxa-1,15,17,21-tetraazapentacyclo...)
Affinity DataIC50:  0.660nMAssay Description:Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50115914(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50:  0.680nMAssay Description:Inhibition of geranyl-geranylation of C-terminal CAAX sequence of Rap 1a in PSN-1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM34539(US8546434, 13)
Affinity DataIC50:  0.690nMAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103306(US8546434, 3)
Affinity DataIC50:  0.740nMpH: 7.5 T: 2°CAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237306(CHEMBL4076352)
Affinity DataIC50:  0.800nMAssay Description:Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223454(6-(3-aminopropyl)-4-(2-chlorophenyl)-9-(1H-pyrazol...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103309(US8546434, 6)
Affinity DataIC50:  0.830nMpH: 7.5 T: 2°CAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103305(US8546434, 2)
Affinity DataIC50:  0.830nMpH: 7.5 T: 2°CAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
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 DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50115928(4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-pipe...)
Affinity DataIC50:  0.850nMAssay Description:The concentration required to displace 50% of a highly potent radiolabeled FPTase inhibitorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50139195(4-(2,2-dimethyl-1,3-dioxolan-4-ylmethyl)-23-oxo-8-...)
Affinity DataIC50:  0.860nMAssay Description:Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM34538(US8546434, 12)
Affinity DataIC50:  0.870nMAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237302(CHEMBL4101697)
Affinity DataIC50:  0.900nMAssay Description:Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM34536(US8546434, 10)
Affinity DataIC50:  0.900nMAssay Description:In vitro activity assay using KSP.More data for this Ligand-Target Pair
In DepthDetails US Patent
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