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TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075926(3-(3-Methoxy-4-pyrrolidin-1-ylmethyl-benzyl)-2-[4-...)
Affinity DataKi:  0.300nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075934(2-[4-(2-Amino-3-hydroxy-propoxy)-phenyl]-3-(3-meth...)
Affinity DataKi:  0.400nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075928(3-(3-Methoxy-4-pyrrolidin-1-ylmethyl-benzyl)-2-[6-...)
Affinity DataKi:  0.5nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075937(2-{4-[2-(2-Hydroxymethyl-pyrrolidin-1-yl)-ethoxy]-...)
Affinity DataKi:  0.5nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075938(3-(3-Methoxy-4-pyrrolidin-1-ylmethyl-benzyl)-2-[4-...)
Affinity DataKi:  0.900nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075932(2-(1,1-Dioxo-1lambda*6*-thiomorpholin-4-yl)-N-{4-[...)
Affinity DataKi:  0.900nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075935(3-(3-Methyl-4-pyrrolidin-1-ylmethyl-benzyl)-2-[4-(...)
Affinity DataKi:  1.90nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075931(3-(3-BROMO-4-PYRROLIDIN-1-YLMETHYL-BENZYL)-2-[4-PY...)
Affinity DataKi:  2.10nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075939(2-Dimethylamino-N-{4-[6-hydroxy-3-(3-methoxy-4-pyr...)
Affinity DataKi:  2.30nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075927(2-[4-(2-Amino-ethoxy)-phenyl]-3-(3-methoxy-4-pyrro...)
Affinity DataKi:  3.80nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075930(2-[4-(2-Pyrrolidin-1-yl-ethoxy)-phenyl]-3-(4-pyrro...)
Affinity DataKi:  4.10nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075933(2-[4-(2-Amino-ethyl)-phenyl]-3-(3-methoxy-4-pyrrol...)
Affinity DataKi:  5.10nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075941(3-(3-Hydroxy-4-pyrrolidin-1-ylmethyl-benzyl)-2-[4-...)
Affinity DataKi:  5.10nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50228863((S)-1-((R)-2-Methylamino-3-phenyl-propionyl)-pyrro...)
Affinity DataKi:  5.5nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075929(2-Amino-N-{4-[6-hydroxy-3-(3-methoxy-4-pyrrolidin-...)
Affinity DataKi:  7nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075940(5-{6-Hydroxy-2-[4-(2-pyrrolidin-1-yl-ethoxy)-pheny...)
Affinity DataKi:  7.20nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProthrombin(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50075936(3-(3-Aminomethyl-4-pyrrolidin-1-ylmethyl-benzyl)-2...)
Affinity DataKi:  11nMAssay Description:Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003355(5-(4-Hexylsulfanyl-[1,2,5]thiadiazol-3-yl)-1-methy...)
Affinity DataIC50:  0.00100nMAssay Description:Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferensMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003363(1-Methyl-5-(4-pentylsulfanyl-[1,2,5]thiadiazol-3-y...)
Affinity DataIC50:  0.00200nMAssay Description:Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferensMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003366(1-Methyl-5-(4-pentyloxy-[1,2,5]thiadiazol-3-yl)-1,...)
Affinity DataIC50:  0.00400nMAssay Description:Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferensMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003359(5-(4-Hexyloxy-[1,2,5]thiadiazol-3-yl)-1-methyl-1,2...)
Affinity DataIC50:  0.00800nMAssay Description:Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferensMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human ADAMTS-5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCollagenase 3(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human MMP13 using Mca-PQG1 peptide substrate assessed as substrate cleavage after 2 to 4 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human ADAMTS-4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003351(3-(4-butoxy-1,2,5-thiadiazol-3-yl)-1-methyl-1,2,5,...)
Affinity DataIC50:  1.40nMAssay Description:Displacement of [3H]-oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003369(1-Methyl-5-(4-propoxy-[1,2,5]thiadiazol-3-yl)-1,2,...)
Affinity DataIC50:  1.60nMAssay Description:In vitro binding affinity against rat hippocampus Muscarinic acetylcholine receptor M1 using [3H]-oxotremorine-M (Oxo-M) as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535210(CHEMBL4448598)
Affinity DataIC50: <1.70nMAssay Description:Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535210(CHEMBL4448598)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA level after 3 hrs by mass spectrometric analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535213(CHEMBL4453084)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003363(1-Methyl-5-(4-pentylsulfanyl-[1,2,5]thiadiazol-3-y...)
Affinity DataIC50:  2.40nMAssay Description:Displacement of [3H]-oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535214(CHEMBL4549771)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535215(CHEMBL4476558)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003351(3-(4-butoxy-1,2,5-thiadiazol-3-yl)-1-methyl-1,2,5,...)
Affinity DataIC50:  3nMAssay Description:Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferensMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetStromelysin-1(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human MMP3 using Mca-PQG1 peptide substrate assessed as substrate cleavage after 2 to 4 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003366(1-Methyl-5-(4-pentyloxy-[1,2,5]thiadiazol-3-yl)-1,...)
Affinity DataIC50:  4nMAssay Description:Displacement of [3H]-pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535212(CHEMBL4569141)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003366(1-Methyl-5-(4-pentyloxy-[1,2,5]thiadiazol-3-yl)-1,...)
Affinity DataIC50:  4nMAssay Description:Displacement of [3H]-pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50033808(CHEMBL3358158)
Affinity DataIC50:  4nMAssay Description:Inhibition of human ADAMTS-4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50033808(CHEMBL3358158)
Affinity DataIC50:  4nMAssay Description:Inhibition of human ADAMTS-5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003363(1-Methyl-5-(4-pentylsulfanyl-[1,2,5]thiadiazol-3-y...)
Affinity DataIC50:  4.80nMAssay Description:Displacement of [3H]-oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535220(CHEMBL4454442)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003355(5-(4-Hexylsulfanyl-[1,2,5]thiadiazol-3-yl)-1-methy...)
Affinity DataIC50:  5nMAssay Description:Displacement of [3H]-pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetDipeptidyl peptidase 4(Human)
Eli Lilly

LigandPNGBDBM15471(4-[(1-{[2-oxo-2-(thiophen-3-yl)ethyl]amino}cyclope...)
Affinity DataIC50:  5nMpH: 7.5 T: 22°CAssay Description:The DPP activity resulted in the formation of the fluorescent product amidomethylcoumarin (AMC), which was monitored by excitation at 355 nm and meas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50033806(CHEMBL3358156)
Affinity DataIC50:  5nMAssay Description:Inhibition of human ADAMTS-4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target72 kDa type IV collagenase(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human MMP2 using Mca-PQG1 peptide substrate assessed as substrate cleavage after 2 to 4 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003351(3-(4-butoxy-1,2,5-thiadiazol-3-yl)-1-methyl-1,2,5,...)
Affinity DataIC50:  5nMAssay Description:Displacement of [3H]-pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003365(3-(3-(ethoxy)-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetra...)
Affinity DataIC50:  5.70nMAssay Description:Displacement of [3H]-oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535215(CHEMBL4476558)
Affinity DataIC50:  6nMAssay Description:Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA level after 3 hrs by mass spectrometric analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetMuscarinic acetylcholine receptor M1(Rat)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50003356(5-(4-Heptyloxy-[1,2,5]thiadiazol-3-yl)-1-methyl-1,...)
Affinity DataIC50:  6.20nMAssay Description:In vitro binding affinity against rat hippocampus M1 receptor using [3H]-pirenzepine (Pz) as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEctonucleotide pyrophosphatase/phosphodiesterase family member 2(Human)
Lilly Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50535213(CHEMBL4453084)
Affinity DataIC50:  6.30nMAssay Description:Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA level after 3 hrs by mass spectrometric analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

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