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Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
Ligand
BDBM50569941
Substrate
n/a
Meas. Tech.
ChEMBL_2110747 (CHEMBL4819597)
IC50
68±n/a nM
Citation
 Guragossian, N; Belhani, B; Moreno, A; Nunes, MT; Gonzalez-Lobato, L; Marminon, C; Berthier, L; Rocio Andrade Pires, AD; Özvegy-Laczka, C; Sarkadi, B; Terreux, R; Bouaziz, Z; Berredjem, M; Jose, J; Di Pietro, A; Falson, P; Le Borgne, M Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2. Eur J Med Chem 211:0 (2021) [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:
BDBM50569941
Synonyms:
CHEMBL4861832
Type:
Small organic molecule
Emp. Form.:
C50H42N2O6
Mol. Mass.:
766.8783
SMILES:
COc1cccc(CCn2c3-c4ccccc4C(=O)c3c3c(OCCOc4ccc5C(=O)c6c7c(CC(C)CC7=O)n(CCc7ccccc7)c6-c5c4)cccc23)c1
Structure:
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