RXP470.1 | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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RXP470.1
Ligand Activity Charts

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] There should be some charts here, you may need to enable JavaScript!
Angiotensin-converting enzyme in Human [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821] There should be some charts here, you may need to enable JavaScript!
MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] There should be some charts here, you may need to enable JavaScript!
MMP10/Matrix metalloproteinase 10 in Human [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238] There should be some charts here, you may need to enable JavaScript!
MMP11/Matrix metalloproteinase 11 in Human [ChEMBL: CHEMBL2867] [GtoPdb: 1635] [UniProtKB: P24347] There should be some charts here, you may need to enable JavaScript!
MMP12/Matrix metalloproteinase 12 in Human [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900] There should be some charts here, you may need to enable JavaScript!
MMP13/Matrix metalloproteinase 13 in Human [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] There should be some charts here, you may need to enable JavaScript!
MMP14/Matrix metalloproteinase 14 in Human [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] There should be some charts here, you may need to enable JavaScript!
MMP2/Matrix metalloproteinase-2 in Human [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] There should be some charts here, you may need to enable JavaScript!
MMP3/Matrix metalloproteinase 3 in Human [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] There should be some charts here, you may need to enable JavaScript!
MMP7/Matrix metalloproteinase 7 in Human [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] There should be some charts here, you may need to enable JavaScript!
MMP8/Matrix metalloproteinase 8 in Human [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] There should be some charts here, you may need to enable JavaScript!
MMP9/Matrix metalloproteinase 9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] There should be some charts here, you may need to enable JavaScript!
Neutral endopeptidase/Neprilysin in Human [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473] There should be some charts here, you may need to enable JavaScript!

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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]