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 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]
