GI254023X [Ligand Id: 9687] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1229516 |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
