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Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
Ligand
BDBM50242177
Substrate
n/a
Meas. Tech.
ChEMBL_639647 (CHEMBL1175385)
IC50
12800±n/a nM
Citation
 Bokesch, HR; Cartner, LK; Fuller, RW; Wilson, JA; Henrich, CJ; Kelley, JA; Gustafson, KR; McMahon, JB; McKee, TC Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids. Bioorg Med Chem Lett 20:3848-50 (2010) [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:
BDBM50242177
Synonyms:
5,8-dihydroxy-10-methoxy-2-methyl-4H-benzo[h]chromen-4-one | 5,8-dihydroxy-10-methoxy-2-propyl-4H-benzo[h]chromen-4-one | CHEMBL454794 | TMC-256C1
Type:
Small organic molecule
Emp. Form.:
C15H12O5
Mol. Mass.:
272.2528
SMILES:
COc1cc(O)cc2cc(O)c3c(oc(C)cc3=O)c12
Structure:
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