Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
Ligand
BDBM50429667
Substrate
n/a
Meas. Tech.
ChEMBL_946239 (CHEMBL2344977)
EC50
18±n/a nM
Citation
 Contino, MZinzi, LPerrone, MGLeopoldo, MBerardi, FPerrone, RColabufo, NA Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp. Bioorg Med Chem Lett 23:1370-4 (2013) [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:
BDBM50429667
Synonyms:
CHEMBL2335007
Type:
Small organic molecule
Emp. Form.:
C32H29N3O4S
Mol. Mass.:
551.655
SMILES:
COc1cc2CCN(Cc3ccc(Oc4ccc(cn4)-c4nc(cs4)-c4cccc(O)c4)cc3)Cc2cc1OC
Structure:
Search PDB for entries with ligand similarity: