Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 38 hits for monomerid = 16592,16594,16595,16596,256500,256502,16592,16594,16595,16596,256500,256502   

TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 0.670nMpH: 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
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 0.670nMAssay Description:Inhibition of MMP13 (unknown origin) using acetyl-Pro-Leu-Gly-[2-mercapto-4-methylpentanoyl]-Leu-Gly-O-ethyl ester as substrate by microplate reader ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 4.80nMAssay Description:Inhibition of recombinant human MMP13 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 8nMAssay Description:Inhibition of human MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 8nMpH: 7.5 T: 2°CAssay Description:MMP-13 was assayed its proteolytic activity using a quenched fluorogenic substrate. The substrate hydrolysis was monitored by recording the increase ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/17/2007
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 8nMAssay Description:Inhibition of MMP13 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 8nMAssay Description:Inhibition of MMP13 (unknown origin) using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 15 mins followed by substrat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 8nMAssay Description:Inhibition of MMP13 (unknown origin) using APMA as substrate preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 8nMAssay Description:Inhibition of human recombinant MMP13 expressed in Escherichia coliMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 70nMAssay Description:Inhibition of full-length recombinant human MMP-13 assessed as bovine type-2 collagen hydrolysis after 18 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16595(4-N,6-N-bis[(3-methylphenyl)methyl]pyrimidine-4,6-...)
Affinity DataIC50: 72nMpH: 7.5 T: 2°CAssay Description:MMP-13 was assayed its proteolytic activity using a quenched fluorogenic substrate. The substrate hydrolysis was monitored by recording the increase ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/17/2007
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16595(4-N,6-N-bis[(3-methylphenyl)methyl]pyrimidine-4,6-...)
Affinity DataIC50: 72nMAssay Description:Inhibition of human MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM256502(US9505743, 70)
Affinity DataIC50: 100nMpH: 7.6 T: 2°CAssay Description:MMP-13 inhibitor activity of the MMP inhibitors of the present invention was measured using the method of Knight (Knight, C. G. et. al, FEBS LETT. 29...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2017
Entry Details
US Patent

TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 100nMpH: 7.6 T: 2°CAssay Description:MMP-13 inhibitor activity of the MMP inhibitors of the present invention was measured using the method of Knight (Knight, C. G. et. al, FEBS LETT. 29...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2017
Entry Details
US Patent

TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 100nMpH: 7.6 T: 2°CAssay Description:MMP-13 inhibitor activity of the MMP inhibitors of the present invention was measured using the method of Knight (Knight, C. G. et. al, FEBS LETT. 29...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2017
Entry Details
US Patent

TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 110nMAssay Description:Non-competitive inhibition of full-length recombinant human MMP-13 assessed as fTHP-15 substrate hydrolysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16594(CHEMBL468901 | N,N -dibenzylpyrimidine-4,6-dicarbo...)
Affinity DataIC50: 400nMAssay Description:Inhibition of human MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16594(CHEMBL468901 | N,N -dibenzylpyrimidine-4,6-dicarbo...)
Affinity DataIC50: 400nMpH: 7.5 T: 2°CAssay Description:MMP-13 was assayed its proteolytic activity using a quenched fluorogenic substrate. The substrate hydrolysis was monitored by recording the increase ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/17/2007
Entry Details Article
PubMed
TargetStromelysin-2(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of recombinant human MMP10 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16592(4-N,6-N-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dica...)
Affinity DataIC50: 6.60E+3nMAssay Description:Inhibition of human MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16592(4-N,6-N-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dica...)
Affinity DataIC50: 6.60E+3nMAssay Description:Inhibition of MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCollagenase 3(Human)
French Alternative Energies and Atomic Energy Commission

LigandPNGBDBM16592(4-N,6-N-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dica...)
Affinity DataIC50: 6.60E+3nMpH: 7.5 T: 2°CAssay Description:MMP-13 was assayed its proteolytic activity using a quenched fluorogenic substrate. The substrate hydrolysis was monitored by recording the increase ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/17/2007
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCytochrome P450 2C19(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin) using (S)-mephentoin substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin) using dextromethophan substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 2C8(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2C8 (unknown origin) using amodiaquine substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin) using diclofenac substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin) using tacrin substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 2B6(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2B6 (unknown origin) using bupropion substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin) using midazolam substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Translational Research Institute

Curated by ChEMBL
LigandPNGBDBM16596(N,N -bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-di...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin) using testosterone substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2016
Entry Details Article
PubMed
TargetMatrix metalloproteinase-9(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 7.40E+4nMAssay Description:Inhibition of recombinant human MMP9 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetNeutrophil collagenase(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 9.80E+4nMAssay Description:Inhibition of recombinant human MMP8 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of recombinant human MMP12 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetMatrilysin(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of recombinant human MMP7 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetStromelysin-1(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of recombinant human MMP3 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
Target72 kDa type IV collagenase(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of recombinant human MMP2 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetInterstitial collagenase(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of recombinant human MMP1 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetMatrix metalloproteinase-14(Human)
Bolderbiopath

Curated by ChEMBL
LigandPNGBDBM256500(BDBM256501 | US9505743, 44)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of recombinant human MMP14 using QXL520-gamma-Abu-Pro-Cha-Abu-Smc-His-Ala-Dab(5-FAM)-Ala-Lys-NH2 as substrate measured every 5 mins for 2 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed