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Found 54 Enz. Inhib. hit(s) with all data for entry = 50018238
TargetCyclin-dependent kinase 2(Homo sapiens (Human))TBA
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.0900nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4(Homo sapiens (Human))TBA
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.130nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 6(Homo sapiens (Human))TBA
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.160nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))TBA
LigandPNGBDBM50446130(AG-014699 | AG-14447 | RUCAPARIB CAMSYLATE | Rucap...)
Affinity DataKi:  2.90nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))TBA
LigandPNGBDBM209932(2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-...)
Affinity DataKi:  2.90nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))TBA
LigandPNGBDBM209932(2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-...)
Affinity DataKi:  5.20nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetDual specificity protein kinase TTK(Homo sapiens (Human))TBA
LigandPNGBDBM532292(JGS79C | N-(2,6-diethylphenyl)-2-[2-methoxy-4-(4-m...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))TBA
LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))TBA
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4(Homo sapiens (Human))TBA
LigandPNGBDBM50110183(Abemaciclib | LY-2835219 | US10626107, Example LY2...)
Affinity DataIC50:  2nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))TBA
LigandPNGBDBM378887(US10266537, Compound 31)
Affinity DataIC50:  2nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))TBA
LigandPNGBDBM50407812(KW-2450 | Kw-2450)
Affinity DataIC50: <2nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
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TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))TBA
LigandPNGBDBM50407812(KW-2450 | Kw-2450)
Affinity DataIC50: <2nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
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TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))TBA
LigandPNGBDBM50088378(Afinitor | Afinitor Disperz | CHEBI:68478 | Everol...)
Affinity DataIC50:  5nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))TBA
LigandPNGBDBM50313650(8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]tr...)
Affinity DataIC50:  5nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))TBA
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetGamma-secretase-activating protein(Homo sapiens (Human))TBA
LigandPNGBDBM50458159(Nirogacestat | PF 03084014 | PF 3084014 | PF-03084...)
Affinity DataIC50:  6.20nMAssay Description:Inhibitory activity against FAAH in Wistar rat brain homogenateMore data for this Ligand-Target Pair
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TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))TBA
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.80nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
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TargetEpidermal growth factor receptor(Homo sapiens (Human))TBA
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  10nMAssay Description:Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 6(Homo sapiens (Human))TBA
LigandPNGBDBM50110183(Abemaciclib | LY-2835219 | US10626107, Example LY2...)
Affinity DataIC50:  10nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4(Homo sapiens (Human))TBA
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  10nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCell division cycle 7-related protein kinase(Homo sapiens (Human))TBA
LigandPNGBDBM27344(2-(pyridin-4-yl)-1H,4H,5H,6H,7H-pyrrolo[3,2-c]pyri...)
Affinity DataIC50:  10nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 2(Homo sapiens (Human))TBA
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  10nMAssay Description:Inhibitory activity against FAAH in Wistar rat brain homogenateMore data for this Ligand-Target Pair
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TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))TBA
LigandPNGBDBM378887(US10266537, Compound 31)
Affinity DataIC50:  12nMAssay Description:Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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TargetRAC-beta serine/threonine-protein kinase(Homo sapiens (Human))TBA
LigandPNGBDBM50313650(8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]tr...)
Affinity DataIC50:  12nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50407809(CHEMBL5095897)
Affinity DataIC50:  13nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
LigandPNGBDBM378887(US10266537, Compound 31)
Affinity DataIC50:  19nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))TBA
LigandPNGBDBM378887(US10266537, Compound 31)
Affinity DataIC50:  22nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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TargetCyclin-dependent kinase 1(Homo sapiens (Human))TBA
LigandPNGBDBM5655(2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydr...)
Affinity DataIC50:  30nMAssay Description:Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleMore data for this Ligand-Target Pair
In DepthDetails PubMedDrugBank

TargetCyclin-dependent kinase 9(Homo sapiens (Human))TBA
LigandPNGBDBM27344(2-(pyridin-4-yl)-1H,4H,5H,6H,7H-pyrrolo[3,2-c]pyri...)
Affinity DataIC50:  34nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 6(Homo sapiens (Human))TBA
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  39nMAssay Description:Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleMore data for this Ligand-Target Pair
LigandPNGBDBM50380363(CHEMBL2017974 | US10173995, Compound 1)
Affinity DataIC50:  50nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
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TargetRAC-gamma serine/threonine-protein kinase(Homo sapiens (Human))TBA
LigandPNGBDBM50313650(8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]tr...)
Affinity DataIC50:  65nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetAurora kinase B(Homo sapiens (Human))TBA
LigandPNGBDBM50407812(KW-2450 | Kw-2450)
Affinity DataIC50:  66nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))TBA
LigandPNGBDBM50536941(CHEMBL4521985)
Affinity DataIC50:  79nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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TargetCyclin-dependent kinase 4(Homo sapiens (Human))TBA
LigandPNGBDBM5655(2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydr...)
Affinity DataIC50:  100nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50380363(CHEMBL2017974 | US10173995, Compound 1)
Affinity DataIC50:  116nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
LigandPNGBDBM50380363(CHEMBL2017974 | US10173995, Compound 1)
Affinity DataIC50:  166nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))TBA
LigandPNGBDBM5655(2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydr...)
Affinity DataIC50:  170nMAssay Description:Inhibitory activity against FAAH in Wistar rat brain homogenateMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetAurora kinase A(Homo sapiens (Human))TBA
LigandPNGBDBM50407812(KW-2450 | Kw-2450)
Affinity DataIC50:  215nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50380363(CHEMBL2017974 | US10173995, Compound 1)
Affinity DataIC50:  262nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
TargetAurora kinase B(Homo sapiens (Human))TBA
LigandPNGBDBM50407812(KW-2450 | Kw-2450)
Affinity DataIC50:  272nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetAurora kinase B(Homo sapiens (Human))TBA
LigandPNGBDBM50407812(KW-2450 | Kw-2450)
Affinity DataIC50:  478nMAssay Description:Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleMore data for this Ligand-Target Pair
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LigandPNGBDBM50365262((+)-JQ1 | (S)-JQ1 (1) | CHEMBL1957266 | JQ1 | US10...)
Affinity DataIC50:  500nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))TBA
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  3.00E+3nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))TBA
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  3.00E+3nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))TBA
LigandPNGBDBM50407810(CHEMBL5289804)
Affinity DataIC50:  3.23E+3nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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LigandPNGBDBM50391802((3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl...)
Affinity DataIC50:  4.20E+3nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetEukaryotic elongation factor 2 kinase(Homo sapiens (Human))TBA
LigandPNGBDBM166686(2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-di...)
Affinity DataIC50:  8.20E+3nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
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TargetThioredoxin(Homo sapiens (Human))TBA
LigandPNGBDBM50407811(CHEMBL5290420)
Affinity DataIC50:  1.00E+4nMAssay Description:Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayMore data for this Ligand-Target Pair
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