Reaction Details |
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Target | Heparanase |
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Ligand | BDBM50466651 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1793531 (CHEMBL4265450) |
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IC50 | 180±n/a nM |
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Citation | Messore, A; Madia, VN; Pescatori, L; Saccoliti, F; Tudino, V; De Leo, A; Bortolami, M; De Vita, D; Scipione, L; Pepi, F; Costi, R; Rivara, S; Scalvini, L; Mor, M; Ferrara, FF; Pavoni, E; Roscilli, G; Cassinelli, G; Milazzo, FM; Battistuzzi, G; Di Santo, R; Giannini, G Novel Symmetrical Benzazolyl Derivatives Endowed with Potent Anti-Heparanase Activity. J Med Chem61:10834-10859 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Heparanase |
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Name: | Heparanase |
Synonyms: | Endo-glucoronidase | HEP | HPA | HPA1 | HPR1 | HPSE | HPSE1 | HPSE_HUMAN | HSE1 | Heparanase 50 kDa subunit | Heparanase 8 kDa subunit | Heparanase-1 |
Type: | PROTEIN |
Mol. Mass.: | 61167.67 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_327900 |
Residue: | 543 |
Sequence: | MLLRSKPALPPPLMLLLLGPLGPLSPGALPRPAQAQDVVDLDFFTQEPLHLVSPSFLSVT
IDANLATDPRFLILLGSPKLRTLARGLSPAYLRFGGTKTDFLIFDPKKESTFEERSYWQS
QVNQDICKYGSIPPDVEEKLRLEWPYQEQLLLREHYQKKFKNSTYSRSSVDVLYTFANCS
GLDLIFGLNALLRTADLQWNSSNAQLLLDYCSSKGYNISWELGNEPNSFLKKADIFINGS
QLGEDFIQLHKLLRKSTFKNAKLYGPDVGQPRRKTAKMLKSFLKAGGEVIDSVTWHHYYL
NGRTATKEDFLNPDVLDIFISSVQKVFQVVESTRPGKKVWLGETSSAYGGGAPLLSDTFA
AGFMWLDKLGLSARMGIEVVMRQVFFGAGNYHLVDENFDPLPDYWLSLLFKKLVGTKVLM
ASVQGSKRRKLRVYLHCTNTDNPRYKEGDLTLYAINLHNVTKYLRLPYPFSNKQVDKYLL
RPLGPHGLLSKSVQLNGLTLKMVDDQTLPPLMEKPLRPGSSLGLPAFSYSFFVIRNAKVA
ACI
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BDBM50466651 |
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n/a |
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Name | BDBM50466651 |
Synonyms: | CHEMBL4283251 |
Type | Small organic molecule |
Emp. Form. | C31H20F2N4O7 |
Mol. Mass. | 598.5099 |
SMILES | OC(=O)Cc1ccc2oc(nc2c1)-c1ccc(NC(=O)Nc2ccc(cc2F)-c2nc3cc(CC(O)=O)ccc3o2)c(F)c1 |
Structure |
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