aldumastat [Ligand Id: 12778] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4650334 (Aldumastat, G-504572, G504572, Glpg1972, GLPG-1972, GLPG1972, S-201086, S201086) |
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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 human recombinant TACE (AA34 to 660) assessed as cleavage of fluorescent substrate using 5FAM-LAQAVRSSSRK-5TAMRA as substrate by biochemical assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ADAMTS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5133] [GtoPdb: 1674] [UniProtKB: Q9UHI8] | ||||||||
| ChEMBL | Inhibition of human recombinant ADAMTS-1 (AA253 to 734) assessed as cleavage of fluorescent substrate using 5(6)-fluorescein-NH-AELQGRPISIAK-5(6)-TAMRA as substrate incubated for 120 mins by biochemical assay | B | 5.46 | pIC50 | >3460 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ADAMTS4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2318] [GtoPdb: 1677] [UniProtKB: O75173] | ||||||||
| ChEMBL | Inhibition of human recombinant ADAMTS-4 (AA1 to 520) assessed as cleavage of fluorescent substrate using as TBIS-1 substrate incubated for 180 mins by biochemical assay | B | 6.81 | pIC50 | 156 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ADAMTS5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2285] [GtoPdb: 1678] [UniProtKB: Q9UNA0] | ||||||||
| ChEMBL | Inhibition of full-length human ADAMTS-5 expressed in HEK293-6E cells using AGC incubated for 50 mins by ELISA | B | 7.2 | pIC50 | 63 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ChEMBL | Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assay | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ADAMTS13/A disintegrin and metalloproteinase with thrombospondin motifs 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2346492] [GtoPdb: 1685] [UniProtKB: Q76LX8] | ||||||||
| ChEMBL | Inhibition of ADAMTS13 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ADAMTS5 in Human [GtoPdb: 1678] [UniProtKB: Q9UNA0] | ||||||||
| GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| ADAMTS5/A disintegrin and metalloproteinase with thrombospondin motifs 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879523] [GtoPdb: 1678] [UniProtKB: Q9R001] | ||||||||
| ChEMBL | Inhibition of ADAMTS-5 in C57BL/6 mouse femoral head cartilage assessed as reduction in IL-1alpha stimulated glycosaminoglycan release measured after 3 days | B | 5.82 | pIC50 | <1500 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP14 (AA112 to 298) assessed as cleavage of fluorescent substrate using 390 MMP FRET as substrate incubated for 30 mins by biochemical assay | B | 5.5 | pIC50 | >3198 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP2 (AA34 to 660) assessed as cleavage of fluorescent substrate using 390 MMP FRET as substrate incubated for 30 mins by biochemical assay | B | 5.94 | pIC50 | 1158 | nM | IC50 | J Med Chem (2021) 64: 2937-2952 [PMID:33719441] |
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]
