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Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
Ligand
BDBM50386737
Substrate
n/a
Meas. Tech.
ChEMBL_826625 (CHEMBL2050879)
IC50
450±n/a nM
Citation
 Valdameri, G; Gauthier, C; Terreux, R; Kachadourian, R; Day, BJ; Winnischofer, SM; Rocha, ME; Frachet, V; Ronot, X; Di Pietro, A; Boumendjel, A Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity. J Med Chem 55:3193-200 (2012) [PubMed]  Article 
Target
Name:
Broad substrate specificity ATP-binding cassette transporter ABCG2
Synonyms:
ABCG2 | ABCG2_HUMAN | ABCP | ATP-Binding Cassette Transporter ABCG2 | ATP-binding cassette sub-family G member 2 | ATP-binding cassette transporter (ABCG2) | ATP-binding cassette, sub-family G, member 2 | BCRP | BCRP1 | Breast cancer resistance protein | CDw338 | MXR | Mitoxantrone resistance-associated protein | Placenta-specific ATP-binding cassette transporter | Urate exporter
Type:
Multi-pass membrane protein; monomer or homodimer; disulfide-linked
Mol. Mass.:
72329.48
Organism:
Homo sapiens (Human)
Description:
Q9UNQ0
Residue:
655
Sequence:
MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVEKEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCNSGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGTQFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIFSIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIINGDSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKKITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDSTGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLPMRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLLMTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGNNPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
  
Inhibitor
Name:
BDBM50386737
Synonyms:
CHEMBL1834566
Type:
Small organic molecule
Emp. Form.:
C21H21NO4
Mol. Mass.:
351.3957
SMILES:
COc1cc(OC)c(\C=C\C(=O)c2cn(C)c3ccccc23)c(OC)c1
Structure:
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