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Found 1213 with Last Name = 'kelly' and Initial = 'tm'
TargetBombesin receptor subtype-3(RAT)
TBA

Curated by ChEMBL
LigandPNGBDBM50336889((2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]...)
Affinity DataKi:  0.600nMAssay Description:Displacement of [3H]Bag-3 from rat BRS-3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(RAT)
TBA

Curated by ChEMBL
LigandPNGBDBM50336889((2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]...)
Affinity DataKi:  0.600nMAssay Description:Displacement of [3H]Bag-3 from rat BRS-3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Mus musculus)
TBA

Curated by ChEMBL
LigandPNGBDBM50336889((2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]...)
Affinity DataKi:  1.60nMAssay Description:Displacement of [3H]Bag-3 from mouse BRS-3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50336889((2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]...)
Affinity DataKi:  3.70nMAssay Description:Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50336886(1-[4-(2,2-dimethylpropyl)-1H-imidazol-2-yl]-2-[4-(...)
Affinity DataKi:  4.20E+3nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50336885(2-[4-(2,2-dimethylpropyl)-1H-imidazol-2-yl]-1-[4-(...)
Affinity DataKi:  5.90E+3nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50336889((2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]...)
Affinity DataKi: >8.00E+3nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50228403((R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-met...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of human DPP4 preincubated for 30 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assayMore data for this Ligand-Target Pair
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50381917(CHEMBL2023112)
Affinity DataIC50:  0.5nMAssay Description:Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50381918(CHEMBL2023113)
Affinity DataIC50:  0.5nMAssay Description:Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50272468((8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydrox...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50381916(CHEMBL2023111)
Affinity DataIC50:  0.600nMAssay Description:Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394612(CHEMBL2164581)
Affinity DataIC50:  0.700nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50400247(CHEMBL2179918)
Affinity DataIC50:  0.700nMAssay Description:Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394616(CHEMBL2164577)
Affinity DataIC50:  0.760nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50:  0.800nM EC50:  1nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human glucocorticoid receptor alpha by displacement of [3H]-dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394609(CHEMBL2164223)
Affinity DataIC50:  0.900nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50400254(CHEMBL2179911)
Affinity DataIC50:  0.900nMAssay Description:Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50543723(CHEMBL4640512)
Affinity DataIC50:  1nMAssay Description:Inhibition of thrombin (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394613(CHEMBL2164580)
Affinity DataIC50:  1.10nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19207((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50:  1.10nM EC50:  4.40nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394611(CHEMBL2164582)
Affinity DataIC50:  1.20nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50167799(1-(4-fluorophenyl)-4a-methyl-4',5'-divinyl-(4'R,4a...)
Affinity DataIC50:  1.20nMAssay Description:Binding affinity for human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50400257(CHEMBL2179908)
Affinity DataIC50:  1.20nMAssay Description:Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50167799(1-(4-fluorophenyl)-4a-methyl-4',5'-divinyl-(4'R,4a...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of human glucocorticoid receptor alpha isoform More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50272523((11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50381915(CHEMBL2023110)
Affinity DataIC50:  1.40nMAssay Description:Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394615(CHEMBL2164578)
Affinity DataIC50:  1.40nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19224((S)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of human glucocorticoid receptor alpha by displacement of [3H]-dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19208((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50:  1.5nM EC50:  8.60nMAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19224((S)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4...)
Affinity DataIC50:  1.5nM EC50:  6nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50400246(CHEMBL2179473)
Affinity DataIC50:  1.60nMAssay Description:Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394608(CHEMBL2164224)
Affinity DataIC50:  1.70nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM60417(US9051329, Example 1)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of human DPP4 preincubated for 30 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assayMore data for this Ligand-Target Pair
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394617(CHEMBL2164576)
Affinity DataIC50:  1.72nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19199((R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of human glucocorticoid receptor alpha by displacement of [3H]-dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19204(2-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH...)
Affinity DataIC50:  1.90nM EC50:  3nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19199((R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4...)
Affinity DataIC50:  1.90nM EC50:  14.4nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50394610(CHEMBL2164222)
Affinity DataIC50:  1.90nMAssay Description:Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50543691(CHEMBL4646369)
Affinity DataIC50:  2nMAssay Description:Inhibition of thrombin (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50381919(CHEMBL2023114)
Affinity DataIC50:  2.10nMAssay Description:Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19225((R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4...)
Affinity DataIC50:  2.10nM EC50:  5nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50272400((8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydrox...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50167810(1-(4-fluorophenyl)-4',4',4a,6'-tetramethyl-(4aS,6'...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of human glucocorticoid receptor alpha isoform More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50167815(1-(4-fluorophenyl)-4',4',4a,6'-tetramethyl-(4aS,6'...)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of human glucocorticoid receptor alpha isoform More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50400249(CHEMBL2179916)
Affinity DataIC50:  2.20nMAssay Description:Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19231((R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4...)
Affinity DataIC50:  2.30nM EC50:  3nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50272434((11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl...)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBombesin receptor subtype-3(RAT)
TBA

Curated by ChEMBL
LigandPNGBDBM50314969(2-(4-(2-(4-(2,2-dimethylbutyl)-1H-imidazol-2-yl)et...)
Affinity DataIC50:  2.40nMAssay Description:Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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