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Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
Ligand
BDBM50068270
Substrate
n/a
Meas. Tech.
ChEMBL_1995597 (CHEMBL4629492)
IC50
42±n/a nM
Citation
 Wu, CP; Lusvarghi, S; Hsiao, SH; Liu, TC; Li, YQ; Huang, YH; Hung, TH; Ambudkar, SV Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs. J Nat Prod 83:1461-1472 (2020) [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:
BDBM50068270
Synonyms:
(E)-3-(4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one | (E)-3-[5-(1,1-Dimethyl-allyl)-4-hydroxy-2-methoxy-phenyl]-1-(4-hydroxy-phenyl)-propenone | 3-(4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one | 3-[5-((E)-1,1-Dimethyl-allyl)-4-hydroxy-2-methoxy-phenyl]-1-(4-hydroxy-phenyl)-propenone | CHEMBL139702 | Licochalcone A
Type:
Small organic molecule
Emp. Form.:
C21H22O4
Mol. Mass.:
338.397
SMILES:
COc1cc(O)c(cc1\C=C\C(=O)c1ccc(O)cc1)C(C)(C)C=C
Structure:
Search PDB for entries with ligand similarity: