CGS-27023A [Ligand Id: 8846] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267178 (CGS-27023A)
  • 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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  • MMP1 in Human [GtoPdb: 1628] [UniProtKB: P03956]
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  • MMP14 in Human [GtoPdb: 1638] [UniProtKB: P50281]
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  • MMP25 in Human [GtoPdb: 1647] [UniProtKB: Q9NPA2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
ChEMBL Inhibition of recombinant human MMP2 preincubated for 30 mins followed by McaPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition measured by fluorescence assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2018) 28: 2413-2417 [PMID:29921475]
GtoPdb - - 7.6 pIC50 25 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]
MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
ChEMBL Inhibition of recombinant human MMP3 (Tyr18 to Cys477 residues) expressed in mouse myeloma cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2017) 138: 979-992 [PMID:28756264]
ChEMBL Inhibition of recombinant human MMP3 preincubated for 30 mins followed by McaPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition measured by fluorescence assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2018) 28: 2413-2417 [PMID:29921475]
GtoPdb - - 7.8 pIC50 16 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]
MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894]
ChEMBL Inhibition of recombinant human MMP8 (Phe21 to Gly467 residues) expressed in mouse myeloma cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 138: 979-992 [PMID:28756264]
GtoPdb - - 8.11 pIC50 7.7 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]
MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
ChEMBL Inhibition of recombinant human MMP9 preincubated for 30 mins followed by McaPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition measured by fluorescence assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2018) 28: 2413-2417 [PMID:29921475]
ChEMBL Inhibition of recombinant human MMP9 (Ala20 to Asp707 residues) expressed in CHO cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 138: 979-992 [PMID:28756264]
GtoPdb - - 8.32 pIC50 4.8 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]
MMP1 in Human [GtoPdb: 1628] [UniProtKB: P03956]
GtoPdb - - 7.25 pIC50 56 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]
MMP14 in Human [GtoPdb: 1638] [UniProtKB: P50281]
GtoPdb - - 7.64 pIC50 23 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]
MMP25 in Human [GtoPdb: 1647] [UniProtKB: Q9NPA2]
GtoPdb - - 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]