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Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
Ligand
BDBM50595124
Substrate
n/a
Meas. Tech.
ChEMBL_2215588 (CHEMBL5128720)
IC50
200±n/a nM
Citation
 Zattoni, IF; Delabio, LC; Dutra, JP; Kita, DH; Scheiffer, G; Hembecker, M; Pereira, GDS; Moure, VR; Valdameri, G Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. Eur J Med Chem 237:0 (2022) [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:
BDBM50595124
Synonyms:
CHEBI:49960 | Caprelsa | GNF-PF-2188 | NSC-744325 | NSC-760766 | VANDETANIB | Vandetanib | ZD-64 | ZD-6474 | ZD6474 | Zactima
Type:
Small organic molecule
Emp. Form.:
C22H24BrFN4O2
Mol. Mass.:
475.354
SMILES:
COc1cc2c(cc1OCC1CCN(C)CC1)[nH]cn\c2=N/c1ccc(Br)cc1F
Structure:
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