cipemastat [Ligand Id: 6466] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL115653 (Ro-32-03555, Ro-323555000, Cipemastat, Trocade)
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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
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  • MMP13/Matrix metalloproteinase 13 in Human [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452]
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  • MMP14/Matrix metalloproteinase 14 in Human [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
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  • MMP2/Matrix metalloproteinase-2 in Human [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
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  • MMP3/Matrix metalloproteinase 3 in Human [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
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  • MMP9/Matrix metalloproteinase 9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ADAM17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536]
ChEMBL Binding affinity to recombinant TACE B 6.64 pKi 230 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2632-2636 [PMID:16516469]
ChEMBL Inhibition of LPS/interferon gamma-stimulated TNFalpha release from HPBMC F 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 2632-2636 [PMID:16516469]
ChEMBL Inhibition of TACE B 6.64 pIC50 230.3 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
ChEMBL Inhibition of Matrix metalloprotease-1 (MMP1) B 5.15 pKi 7000 nM Ki J. Med. Chem. (2003) 46: 3840-3852 [PMID:12930146]
GtoPdb - - 8.5 pKi 3 nM Ki Ann. Rheum. Dis. (2001) 60 Suppl 3: iii62-7 [PMID:11890658]
ChEMBL Inhibition of matrix metalloprotease-1 (MMP-1). B 8.52 pKi 3 nM Ki J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL Binding affinity to recombinant MMP1 B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2632-2636 [PMID:16516469]
ChEMBL Inhibition of MMP1 B 8.64 pIC50 2.3 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452]
ChEMBL Inhibition of matrix metalloprotease-13 (MMP-13). B 8.52 pKi 3 nM Ki J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL Binding affinity to recombinant MMP13 B 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2632-2636 [PMID:16516469]
ChEMBL Inhibition of MMP13 assessed as dissociation constant B 9.28 pKi 0.53 nM Ki J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
ChEMBL Inhibition of MMP13 in presence of 1% bovine serum albumin B 8.33 pIC50 4.7 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
ChEMBL Inhibition of MMP13 B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
ChEMBL Inhibitory activity against matrix metalloprotease-13 (MMP13) B 8.47 pIC50 3.4 nM IC50 J. Med. Chem. (2003) 46: 3840-3852 [PMID:12930146]
MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
ChEMBL Inhibition of MMP14 B 7.64 pIC50 23 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
ChEMBL Inhibition of matrix metalloprotease-2 (MMP-2). B 6.81 pKi 154 nM Ki J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL Inhibitory activity against matrix metalloprotease-2 (MMP2) B 6.81 pIC50 154 nM IC50 J. Med. Chem. (2003) 46: 3840-3852 [PMID:12930146]
MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
ChEMBL Inhibition of matrix metalloprotease-3 (MMP-3). B 6.28 pKi 527 nM Ki J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL Binding affinity to recombinant MMP3 B 7.25 pKi 56 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2632-2636 [PMID:16516469]
ChEMBL Inhibitory activity against matrix metalloprotease-3 (MMP3) B 6.28 pIC50 527 nM IC50 J. Med. Chem. (2003) 46: 3840-3852 [PMID:12930146]
ChEMBL Inhibition of MMP3 B 7.06 pIC50 87 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237]
ChEMBL Inhibition of MMP7 B 7.73 pIC50 18.5 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]
MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894]
ChEMBL Inhibition of matrix metalloprotease-8 (MMP-8). B 8.4 pKi 4 nM Ki J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
ChEMBL Inhibition of matrix metalloprotease-9 (MMP-9). B 7.23 pKi 59 nM Ki J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL Inhibitory activity against matrix metalloprotease-9 (MMP9) B 7.24 pIC50 58 nM IC50 J. Med. Chem. (2003) 46: 3840-3852 [PMID:12930146]
ChEMBL Inhibition of MMP9 B 8.62 pIC50 2.4 nM IC50 J. Med. Chem. (2009) 52: 3523-3538 [PMID:19422229]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]