GI254023X [Ligand Id: 9687] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1229516
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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
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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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  • 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
ADAM10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5028] [GtoPdb: 1658] [UniProtKB: O14672]
ChEMBL Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA B 4.82 pIC50 15000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA B 4.92 pIC50 12000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA B 4.92 pIC50 12000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA B 4.92 pIC50 12000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA B 5 pIC50 10000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA B 5 pIC50 10000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA B 5 pIC50 10000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA B 5.15 pIC50 7000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
GtoPdb - - 5.28 pIC50 5300 nM IC50 Neurodegener Dis (2010) 7: 232-8 [PMID:20197648]
ChEMBL Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA B 5.3 pIC50 5000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of recombinant human ADAM-10 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate after 1 hr by fluorometric assay B 7.57 pIC50 27 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ADAM17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536]
GtoPdb - - 3.27 pIC50 541000 nM IC50 Neurodegener Dis (2010) 7: 232-8 [PMID:20197648]
ChEMBL Inhibition of ADAM-17 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA B 5 pIC50 10000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of ADAM-17 in human L428 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA B 5 pIC50 10000 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
ChEMBL Inhibition of recombinant human ADAM-17 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate after 30 mins by fluorometric assay B 6.07 pIC50 860 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
ChEMBL Inhibition of human MMP-1 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate after 3 hrs by fluorometric assay B 6.9 pIC50 125 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
ChEMBL Inhibition of recombinant human MMP-14 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate after 3 hrs by fluorometric assay B 7.06 pIC50 88 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
ChEMBL Inhibition of recombinant human MMP-2 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate after 3 hrs by fluorometric assay B 8.68 pIC50 2.1 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]
MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
ChEMBL Inhibition of recombinant human MMP-9 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate after 3 hrs by fluorometric assay B 8.29 pIC50 5.1 nM IC50 Eur. J. Med. Chem. (2016) 111: 193-201 [PMID:26871660]

ChEMBL data shown on this page come from version 28:

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]