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Found 488 with Last Name = 'garbaccio' and Initial = 'rm'
TargetCytochrome P450 3A4(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50169690(CHEMBL3806137)
Affinity DataKi:  540nMAssay Description:Time dependent inhibition of CYP3A4 in human liver microsomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 2B(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50145198(CHEMBL3765778)
Affinity DataKi:  1.90E+3nMAssay Description:Positive allosteric modulation of 5-HT2B receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50145198(CHEMBL3765778)
Affinity DataKi:  2.00E+3nMAssay Description:Positive allosteric modulation of platelet-activating factor receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476583(US10869929, Compound 18 | US11554172, Compound 18)
Affinity DataIC50:  0.100nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476583(US10869929, Compound 18 | US11554172, Compound 18)
Affinity DataIC50:  0.100nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM589245(US11554172, Compound 19)
Affinity DataIC50:  0.140nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476584(US10869929, Compound 19)
Affinity DataIC50:  0.140nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM589230(US11554172, Compound Fluticasone-Propionate)
Affinity DataIC50:  0.150nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50354849(CCI-18781 | Cutivate | FLUTICASONE PROPIONATE | Fl...)
Affinity DataIC50:  0.150nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476575(US10869929, Compound 8 | US11554172, Compound 8)
Affinity DataIC50:  0.25nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476575(US10869929, Compound 8 | US11554172, Compound 8)
Affinity DataIC50:  0.25nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476572(US10869929, Compound 6 | US11554172, Compound 6)
Affinity DataIC50:  0.320nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476572(US10869929, Compound 6 | US11554172, Compound 6)
Affinity DataIC50:  0.320nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195211(2-oxo-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-1...)
Affinity DataIC50:  0.340nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220966(1-[(3R,3aR)-8-fluoro-3-(3-morpholin-4-yl-propyl)-3...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of kinesin spindle proteinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476567(US10869929, Compound 3 | US11554172, Compound 3)
Affinity DataIC50:  0.440nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476567(US10869929, Compound 3 | US11554172, Compound 3)
Affinity DataIC50:  0.440nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476573(US10869929, Compound 7 | US11554172, Compound 7)
Affinity DataIC50:  0.450nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476573(US10869929, Compound 7 | US11554172, Compound 7)
Affinity DataIC50:  0.450nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
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
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220958(1-[(3R,3aR)-3-(3-amino-propyl)-8-fluoro-3-phenyl-3...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of kinesin spindle proteinMore 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195197(6-(isothiazol-4-yl)-3-(5-(piperidin-1-ylmethyl)-1H...)
Affinity DataIC50:  0.640nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195213(3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-6-(1H-p...)
Affinity DataIC50:  0.650nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195198(3-(5-((4-(aminomethyl)piperidin-1-yl)methyl)-1H-in...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476568(US10869929, Compound 4 | US11554172, Compound 4)
Affinity DataIC50:  0.710nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM476568(US10869929, Compound 4 | US11554172, Compound 4)
Affinity DataIC50:  0.710nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195200(3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-6-(1H-1...)
Affinity DataIC50:  0.740nMAssay Description:Inhibition of human CHEK1More 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220324(1-((R)-5-((S)-3-amino-2-fluoropropyl)-3-(2,5-diflu...)
Affinity DataIC50:  0.820nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195218(3-(5-(morpholinomethyl)-1H-indol-2-yl)-6-(1H-pyraz...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50354850(BUDESONIDE | US10869929, Compound Budesonide | US1...)
Affinity DataIC50:  0.900nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
In DepthDetails US PatentDrugBank

TargetTSC22 domain family protein 3(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50354850(BUDESONIDE | US10869929, Compound Budesonide | US1...)
Affinity DataIC50:  0.900nMAssay Description:HUT78 cells were cultured in IMEM plus 20% heat inactivated FBS and cell density was maintained between 0.1 to 1.2 million/mL. 786-O cells were cultu...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220964(1-[3-((3R,3aR)-2-acetyl-8-fluoro-3-phenyl-3a,4-dih...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of kinesin spindle proteinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220326((S)-1-(5-(3-aminopropyl)-3-(2,5-difluorophenyl)-5-...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220320(1-((S)-3-(2,5-difluorophenyl)-5-(3-((S)-3-fluoropy...)
Affinity DataIC50:  1nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220331(1-((S)-5-(3-((1R,4R)-5-oxa-2-aza-bicyclo[2.2.1]hep...)
Affinity DataIC50:  1nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195216(3-(5-((4-fluoropiperidin-1-yl)methyl)-1H-indol-2-y...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223484(6-(3-aminopropyl)-4-(3-hydroxyphenyl)-9-(1H-pyrazo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220967(1-[(3R,3aR)-8-chloro-3-(3-dimethylamino-propyl)-3-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of kinesin spindle proteinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220970(1-[(3R,3aR)-8-methyl-3-(3-morpholin-4-yl-propyl)-3...)
Affinity DataIC50:  1nMAssay Description:Inhibition of kinesin spindle proteinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220969(1-{(3R,3aR)-3-[3-(4-acetyl-piperazin-1-yl)-propyl]...)
Affinity DataIC50:  1nMAssay Description:Inhibition of kinesin spindle proteinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-like protein KIF11(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220332(1-((S)-5-(3-(2-aza-bicyclo[2.2.1]heptan-2-yl)propy...)
Affinity DataIC50:  1nMAssay Description:Inhibition of KSP by ATPase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50220886(5-(3-aminopropyl)-7,8-dicyclohexyl-3-methyl-2H-pyr...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of Chk1 by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50195209(6-(1-methyl-1H-pyrazol-4-yl)-3-(5-(piperidin-1-ylm...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of human CHEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM92404(CHEMBL250843 | PDK1 inhibitor, 5)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of Chk1 by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223473(6-(3-aminopropyl)-4-(4-chlorophenyl)-9-(1H-pyrazol...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50223475(6-(3-aminopropyl)-4-(2,4-dichlorophenyl)-9-(1H-pyr...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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