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Target
Heparanase
Ligand
BDBM50506597
Substrate
n/a
Meas. Tech.
ChEMBL_1826461 (CHEMBL4326335)
IC50
160±n/a nM
Citation
 Madia, VN; Messore, A; Pescatori, L; Saccoliti, F; Tudino, V; De Leo, A; Bortolami, M; Scipione, L; 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 Benzazole Derivatives Endowed with Potent Antiheparanase Activity. J Med Chem 61:6918-6936 (2018) [PubMed]  Article 
Target
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:
MLLRSKPALPPPLMLLLLGPLGPLSPGALPRPAQAQDVVDLDFFTQEPLHLVSPSFLSVTIDANLATDPRFLILLGSPKLRTLARGLSPAYLRFGGTKTDFLIFDPKKESTFEERSYWQSQVNQDICKYGSIPPDVEEKLRLEWPYQEQLLLREHYQKKFKNSTYSRSSVDVLYTFANCSGLDLIFGLNALLRTADLQWNSSNAQLLLDYCSSKGYNISWELGNEPNSFLKKADIFINGSQLGEDFIQLHKLLRKSTFKNAKLYGPDVGQPRRKTAKMLKSFLKAGGEVIDSVTWHHYYLNGRTATKEDFLNPDVLDIFISSVQKVFQVVESTRPGKKVWLGETSSAYGGGAPLLSDTFAAGFMWLDKLGLSARMGIEVVMRQVFFGAGNYHLVDENFDPLPDYWLSLLFKKLVGTKVLMASVQGSKRRKLRVYLHCTNTDNPRYKEGDLTLYAINLHNVTKYLRLPYPFSNKQVDKYLLRPLGPHGLLSKSVQLNGLTLKMVDDQTLPPLMEKPLRPGSSLGLPAFSYSFFVIRNAKVAACI
  
Inhibitor
Name:
BDBM50506597
Synonyms:
CHEMBL4576477
Type:
Small organic molecule
Emp. Form.:
C28H22BrFN4O2
Mol. Mass.:
545.402
SMILES:
COc1ccc(cc1Br)C(=O)Nc1ccc(CNc2ccc(cc2F)-c2nc3ccccc3[nH]2)cc1
Structure:
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