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Report error Found 1133 Enz. Inhib. hit(s) with Target = 'Macrophage metalloelastase'
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360964(CHEMBL1935285)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360965(CHEMBL1935286)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50265078((4S)-5-amino-4-((2S)-2-((2S)-3-((4-bromophenyl)(hy...)
Affinity DataKi:  0.190nMAssay Description:Inhibition of MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50592891(CHEMBL5191016)
Affinity DataKi:  0.190nMAssay Description:Inhibition of human MMP-12 expressed in Escherichia coli BL21(DE3) using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins fo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM92441(RXP470, Compound 4 | RXP470, 1)
Affinity DataKi:  0.190nM ΔG°:  -55.5kJ/molepH: 6.8 T: 2°CAssay Description:Enzyme assay using matrix metalloproteinases.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50299051(N-Hydroxy-2-{2-[4-(4-methoxy-phenoxy)benzenesulfon...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of autoactivated human pro-MMP12 after 4 hrs by fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360967(CHEMBL1935288)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM92441(RXP470, Compound 4 | RXP470, 1)
Affinity DataKi:  0.200nM ΔG°:  -55.4kJ/molepH: 6.8 T: 2°CAssay Description:Enzyme assay using human matrix metalloproteases or ADAMTS.More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/5/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50161330((R)-2-[(Biphenyl-4-sulfonyl)-isopropoxy-amino]-N-h...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of autoactivated human pro-MMP12 after 4 hrs by fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360966(CHEMBL1935287)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50148216(4-[4-(4-Fluoro-phenoxy)-benzenesulfonylamino]-tetr...)
Affinity DataIC50: 0.240nMAssay Description:Inhibition of matrix metalloprotease-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/10/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50265078((4S)-5-amino-4-((2S)-2-((2S)-3-((4-bromophenyl)(hy...)
Affinity DataKi:  0.240nMpH: 6.8Assay Description:Inhibition of human MMP12 catalytic domain (98 to 266) at pH 6.8 by isothermal titration calorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50505154(CHEMBL4581500)
Affinity DataKi:  0.260nMAssay Description:Inhibition of human MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50265078((4S)-5-amino-4-((2S)-2-((2S)-3-((4-bromophenyl)(hy...)
Affinity DataKi:  0.260nMAssay Description:Binding affinity to human MMP12 catalytic domain (98 to 266) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50426080(CHEMBL2316257)
Affinity DataKi:  0.280nMAssay Description:Inhibition of human MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50426080(CHEMBL2316257)
Affinity DataKi:  0.280nMAssay Description:Binding affinity to human MMP12 catalytic domain (98 to 266) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360956(CHEMBL1935304)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM120258(US8691753, 95 bis)
Affinity DataKi:  0.300nMAssay Description:The inhibition tests and the evaluation of the inhibition constants (Ki) on the various MMPs were carried out as described by Devel et al. (Devel et ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/6/2014
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50610465(CHEMBL5288452)
Affinity DataIC50: 0.368nMAssay Description:Inhibition of MMP12 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50295489((S)-2-(8-(Methoxycarbonylamino)dibenzo[b,d]thiophe...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human recombinant MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360968(CHEMBL1935290)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360963(CHEMBL1935284)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50062351((R)-N*4*-Hydroxy-N*1*-[2-(1H-indol-3-yl)-1-methylc...)
Affinity DataIC50: 0.460nMAssay Description:Inhibition of recombinant human MMP12 using MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50610466(CHEMBL5280430)
Affinity DataIC50: 0.566nMAssay Description:Inhibition of MMP12 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360959(CHEMBL1935280)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50299051(N-Hydroxy-2-{2-[4-(4-methoxy-phenoxy)benzenesulfon...)
Affinity DataIC50: 0.850nMAssay Description:Inhibition of autoactivated human pro-MMP12 after 1 hr preincubation by fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50299051(N-Hydroxy-2-{2-[4-(4-methoxy-phenoxy)benzenesulfon...)
Affinity DataIC50: 0.890nMAssay Description:Inhibition of autoactivated human pro-MMP12 after 30 mins preincubation by fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM28480((2S)-3-methyl-2-({12-[(thiophen-3-ylcarbamoyl)amin...)
Affinity DataIC50: 0.900nMpH: 7.5 T: 2°CAssay Description:The assays for human MMP activity were performed by incubating fluorogenic peptide substrate with recombinant human MMP catalytic domain along with v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2009
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50505152(CHEMBL4435285)
Affinity DataKi:  0.900nMAssay Description:Inhibition of human MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50428828(CHEMBL2337131)
Affinity DataIC50: 0.930nMAssay Description:Inhibition of MMP12 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50151732(4-[4-(2,4-Dichloro-benzyloxy)-benzenesulfonyl]-3-h...)
Affinity DataIC50: 0.950nMAssay Description:Inhibition of matrix metalloprotease 12More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50026624(CHEMBL1935289)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50505151(CHEMBL4520279)
Affinity DataKi:  1nMAssay Description:Inhibition of human MMP12 by photoaffinity probe based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360969(CHEMBL1935291)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605508(US11673884, Compound AC-2)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605513(US11673884, Compound AC-6)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MMP12 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopropionyl)-AR-OH as substrate after 2 to 4 hrs by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605512(US11673884, Compound AC-5)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50434226(CHEMBL2385483)
Affinity DataKi:  1nMAssay Description:Inhibition of MMP12 (unknown origin)-mediated Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorimetric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605509(US11673884, Compound AC-3)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605517(US11673884, Compound AC-10)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605516(US11673884, Compound AC-9)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605515(US11673884, Compound AC-8)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50062351((R)-N*4*-Hydroxy-N*1*-[2-(1H-indol-3-yl)-1-methylc...)
Affinity DataIC50: 1nMAssay Description:Inhibition of MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50555050(CHEMBL4764575)
Affinity DataKi:  1nMAssay Description:Inhibition of human recombinant MMP12 using Mca-Lys-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605519(US11673884, Compound AC-12)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM605518(US11673884, Compound AC-11)
Affinity DataIC50: 1nMAssay Description:The inhibitory effect of compounds on the rate of cleaving fluorogenic MMP substrate (Enzo, BML-P128) by recombinant human MMP-12 catalytic domain (E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM120222(US8691753, 71)
Affinity DataKi:  1.05nMAssay Description:The inhibition tests and the evaluation of the inhibition constants (Ki) on the various MMPs were carried out as described by Devel et al. (Devel et ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/6/2014
Entry Details
US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM28481((2S)-3-methyl-2-{[12-({[2-(thiophen-2-yl)ethyl]car...)
Affinity DataIC50: 1.10nMpH: 7.5 T: 2°CAssay Description:The assays for human MMP activity were performed by incubating fluorogenic peptide substrate with recombinant human MMP catalytic domain along with v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2009
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50555052(CHEMBL4751015)
Affinity DataKi:  1.10nMAssay Description:Inhibition of human recombinant MMP12 using Mca-Lys-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
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