RXP470.1 [Ligand Id: 7812] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL507420
  • ADAM17 in Human [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536]
  • This target only has 1 pki data point
  • 4
1 CHEMBL507420_lig_chart_1 ADAM17 Human
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  • Angiotensin-converting enzyme in Human [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821]
  • This target only has 1 pki data point
  • 4
2 CHEMBL507420_lig_chart_2 Angiotensin-converting enzyme Human
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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
  • This target only has 1 pki data point
  • 4.17
3 CHEMBL507420_lig_chart_3 Matrix metalloproteinase-1 Human
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  • MMP10/Matrix metalloproteinase 10 in Human [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238]
  • This target only has 1 pki data point
  • 6.83
4 CHEMBL507420_lig_chart_4 Matrix metalloproteinase 10 Human
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  • MMP11/Matrix metalloproteinase 11 in Human [ChEMBL: CHEMBL2867] [GtoPdb: 1635] [UniProtKB: P24347]
  • This target only has 1 pki data point
  • 4.74
5 CHEMBL507420_lig_chart_5 Matrix metalloproteinase 11 Human
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  • MMP12/Matrix metalloproteinase 12 in Human [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900]
  • 9.6
6 CHEMBL507420_lig_chart_6 Matrix metalloproteinase 12 Human
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  • MMP13/Matrix metalloproteinase 13 in Human [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452]
  • 7.08
7 CHEMBL507420_lig_chart_7 Matrix metalloproteinase 13 Human
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  • MMP14/Matrix metalloproteinase 14 in Human [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
  • This target only has 1 pki data point
  • 6.85
8 CHEMBL507420_lig_chart_8 Matrix metalloproteinase 14 Human
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  • MMP2/Matrix metalloproteinase-2 in Human [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
  • This target only has 1 pki data point
  • 6.72
9 CHEMBL507420_lig_chart_9 Matrix metalloproteinase-2 Human
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  • MMP3/Matrix metalloproteinase 3 in Human [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
  • This target only has 1 pki data point
  • 7.4
10 CHEMBL507420_lig_chart_10 Matrix metalloproteinase 3 Human
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  • MMP7/Matrix metalloproteinase 7 in Human [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237]
  • This target only has 1 pki data point
  • 6.2
11 CHEMBL507420_lig_chart_11 Matrix metalloproteinase 7 Human
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  • MMP8/Matrix metalloproteinase 8 in Human [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894]
  • This target only has 1 pki data point
  • 6.57
12 CHEMBL507420_lig_chart_12 Matrix metalloproteinase 8 Human
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  • MMP9/Matrix metalloproteinase 9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
  • This target only has 1 pki data point
  • 5.9
13 CHEMBL507420_lig_chart_13 Matrix metalloproteinase 9 Human
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  • Neutral endopeptidase/Neprilysin in Human [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
  • This target only has 1 pki data point
  • 4
14 CHEMBL507420_lig_chart_14 Neprilysin Human
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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 Inhibition of TACE B 4 pKi >100000 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
Angiotensin-converting enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821]
ChEMBL Inhibition of ACE B 4 pKi >100000 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
ChEMBL Inhibition of MMP1 B 4.17 pKi 67000 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP10/Matrix metalloproteinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238]
ChEMBL Inhibition of human MMP10 catalytic domain using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 fluorogenic substrate by spectrophotometric analysis B 6.83 pKi 149 nM Ki J Med Chem (2017) 60: 403-414 [PMID:27996256]
MMP11/Matrix metalloproteinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2867] [GtoPdb: 1635] [UniProtKB: P24347]
ChEMBL Inhibition of MMP11 B 4.74 pKi 18400 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP12/Matrix metalloproteinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900]
GtoPdb - - 8.62 pKi 2.4 nM Ki J Med Chem (2013) 56: 1149-59 [PMID:23343195]
ChEMBL Binding affinity to human MMP12 catalytic domain (98 to 266) by isothermal titration calorimetry B 9.59 pKi 0.26 nM Ki J. Med. Chem. (2013) 56: 1149-1159 [PMID:23343195]
ChEMBL Inhibition of human MMP12 catalytic domain (98 to 266) at pH 6.8 by isothermal titration calorimetry B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2013) 56: 1149-1159 [PMID:23343195]
ChEMBL Inhibition of MMP12 B 9.72 pKi 0.19 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452]
ChEMBL Inhibition of human MMP13 catalytic domain using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 fluorogenic substrate by spectrophotometric analysis B 6.86 pKi 139 nM Ki J Med Chem (2017) 60: 403-414 [PMID:27996256]
ChEMBL Inhibition of MMP13 B 7.31 pKi 49 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
ChEMBL Inhibition of MMP14 B 6.85 pKi 140 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
ChEMBL Inhibition of MMP2 B 6.72 pKi 192 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
ChEMBL Inhibition of MMP3 B 7.4 pKi 40 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237]
ChEMBL Inhibition of MMP7 B 6.2 pKi 626 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894]
ChEMBL Inhibition of MMP8 B 6.57 pKi 271 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
ChEMBL Inhibition of MMP9 B 5.9 pKi 1265 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]
Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
ChEMBL Inhibition of NEP B 4 pKi >100000 nM Ki Bioorg. Med. Chem. (2008) 16: 8781-8794 [PMID:18790648]

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]