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Found 586 with Last Name = 'heim' and Initial = 'd'
TargetE3 ubiquitin-protein ligase XIAP [241-356](Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

US Patent
LigandPNGBDBM620168(US20230295181, Compound 81)
Affinity DataKi:  55nMAssay Description:Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase XIAP [241-356](Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

US Patent
LigandPNGBDBM620165(US20230295181, Compound 80)
Affinity DataKi:  55nMAssay Description:Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase XIAP [241-356](Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

US Patent
LigandPNGBDBM620153(US20230295181, Compound 65)
Affinity DataKi:  55nMAssay Description:Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase XIAP [241-356](Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

US Patent
LigandPNGBDBM391840(US10300074, Compd 35 | US20230295181, Compound A)
Affinity DataKi:  55nMAssay Description:Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase XIAP [241-356](Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

US Patent
LigandPNGBDBM620169(US20230295181, Compound 82)
Affinity DataKi:  55nMAssay Description:Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase XIAP [241-356](Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

US Patent
LigandPNGBDBM620148(US20230295181, Compound 38)
Affinity DataKi:  66nMAssay Description:Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201193(CHEMBL3974372)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201194(CHEMBL3932600)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201195(CHEMBL3972792)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201196(CHEMBL3961751)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201197(CHEMBL3895686)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201198(CHEMBL3968104)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201199(CHEMBL3934430)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201200(CHEMBL3905875)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201201(CHEMBL3901708)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201202(CHEMBL3971239)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201203(CHEMBL3905724)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201204(CHEMBL3927537)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201205(CHEMBL3914706)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201206(CHEMBL3960176)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201207(CHEMBL3910734)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201208(CHEMBL3892750)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201209(CHEMBL3914868)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201210(CHEMBL3933745)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201192(CHEMBL3932681)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201191(CHEMBL3951442)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201190(CHEMBL3942705)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201189(CHEMBL3984675)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201188(CHEMBL3891635)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201186(CHEMBL3923732)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBiotin--protein ligase(Homo sapiens (Human))
University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50201187(CHEMBL3976601)
Affinity DataKi: >1.60E+4nMAssay Description:Inhibition of human biotin protein ligase assessed as reduction in 3H-biotin incorporation into pyruvate carboxylase biotin domain after 10 mins by l...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50082053((E)-(1R,9S,12S,13R,17R,21S,23S,24R,25S,27R)-17-Eth...)
Affinity DataIC50:  0.770nMAssay Description:The compound was tested for binding affinity against human FK506 binding protein 12More 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
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
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
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
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
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
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
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
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
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
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