IK-862 [Ligand Id: 8680] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL148169 (IK-682) |
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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] | ||||||||
| GtoPdb | - | - | 9.25 | pKi | 0.56 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-94 [PMID:18790648] |
| ChEMBL | Inhibition of TACE catalytic domain by FRET assay | B | 10.22 | pKi | 0.06 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 54-57 [PMID:19054672] |
| ChEMBL | Inhibition of Tumor necrosis factor alpha secretion in LPS-stimulated human whole blood assay | F | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of pTACE | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2769-2774 [PMID:17368021] |
| ChEMBL | Inhibition of TACE | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2009) 17: 444-459 [PMID:19095454] |
| ChEMBL | Inhibition of TACE | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2009) 17: 444-459 [PMID:19095454] |
| ChEMBL | Inhibition of TACE | B | 9.25 | pIC50 | 0.56 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 34-39 [PMID:17064892] |
| ChEMBL | Inhibition of Tumor necrosis factor alpha secretion in LPS-stimulated human whole blood assay | F | 9.46 | pIC50 | 0.35 | nM | IC50 | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ADAM17 in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3332] [UniProtKB: O77636] | ||||||||
| ChEMBL | Affinity for Tumor necrosis factor alpha converting enzyme (TACE) | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of pig TACE | B | 9.25 | pKi | 0.56 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of porcine TACE | B | 9.25 | pKi | 0.56 | nM | Ki | Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823] |
| ChEMBL | Inhibitory activity against porcine Tumor necrosis factor alpha converting enzyme. | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ADAM33/Disintegrin and metalloproteinase domain-containing protein 33 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6121] [GtoPdb: 1673] [UniProtKB: Q9BZ11] | ||||||||
| GtoPdb | - | - | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-94 [PMID:18790648] |
| ChEMBL | Inhibition of ADAM33 | B | 7.82 | pKi | 15 | 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 | Affinity towards Matrix metalloprotease-1 (MMP-1) | B | 4.52 | pKi | 30000 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of MMP1 | B | 4.52 | pKi | 30000 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of MMP1 | B | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 34-39 [PMID:17064892] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Affinity for Matrix metalloprotease-13 (MMP-13) | B | 5.85 | pKi | 1417 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Binding affinity to MMP13 | B | 5.85 | pKi | 1417 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2769-2774 [PMID:17368021] |
| ChEMBL | Inhibition of MMP13 | B | 5.85 | pKi | 1417 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of MMP13 | B | 5.85 | pIC50 | 1417 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 34-39 [PMID:17064892] |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Affinity for Matrix metalloprotease-14 (MMP-14) | B | 4.8 | pKi | 15872 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of MMP14 | B | 4.8 | pKi | 15872 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP15/Matrix metalloproteinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2963] [GtoPdb: 1639] [UniProtKB: P51511] | ||||||||
| ChEMBL | Affinity for Matrix metalloprotease-15 (MMP-15) | B | 5.4 | pKi | 3997 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of MMP15 | B | 5.4 | pKi | 3997 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP16/Matrix metalloproteinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2200] [GtoPdb: 1640] [UniProtKB: P51512] | ||||||||
| ChEMBL | Affinity for Matrix metalloprotease-16 (MMP-16) | B | 5.8 | pKi | 1599 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of MMP16 | B | 5.8 | pKi | 1599 | 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 | Affinity for Matrix metalloprotease-2 (MMP-2) | B | 5.69 | pKi | 2050 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Binding affinity to MMP2 | B | 5.69 | pKi | 2050 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2769-2774 [PMID:17368021] |
| ChEMBL | Inhibition of MMP2 | B | 5.69 | pKi | 2050 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of MMP2 | B | 5.69 | pIC50 | 2050 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 34-39 [PMID:17064892] |
| MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Affinity for Matrix metalloprotease-3 (MMP-3) | B | 6.85 | pKi | 141 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Binding affinity to MMP3 | B | 6.85 | pKi | 141 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2769-2774 [PMID:17368021] |
| ChEMBL | Inhibition of MMP3 | B | 6.85 | pKi | 141 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of MMP3 | B | 6.85 | pIC50 | 141 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 34-39 [PMID:17064892] |
| MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] | ||||||||
| ChEMBL | Affinity for Matrix metalloprotease-7 (MMP-7) | B | 6.59 | pKi | 259 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Binding affinity to MMP7 | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2769-2774 [PMID:17368021] |
| ChEMBL | Inhibition of MMP7 | B | 6.59 | pKi | 259 | 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 | Affinity for Matrix metalloprotease-8 (MMP-8) | B | 6.59 | pKi | 257 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of MMP8 | B | 6.59 | pKi | 257 | 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 | Affinity towards Matrix metalloprotease-9 (MMP-9) | B | 4.99 | pKi | 10340 | nM | Ki | J Med Chem (2002) 45: 4954-4957 [PMID:12408705] |
| ChEMBL | Inhibition of MMP9 | B | 4.99 | pKi | 10340 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of MMP9 | B | 4.99 | pIC50 | 10340 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 34-39 [PMID:17064892] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
