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Target
Progesterone receptor
Ligand
BDBM50084948
Substrate
n/a
Meas. Tech.
ChEMBL_1519264 (CHEMBL3624761)
IC50
12±n/a nM
Citation
 De Savi, C; Bradbury, RH; Rabow, AA; Norman, RA; de Almeida, C; Andrews, DM; Ballard, P; Buttar, D; Callis, RJ; Currie, GS; Curwen, JO; Davies, CD; Donald, CS; Feron, LJ; Gingell, H; Glossop, SC; Hayter, BR; Hussain, S; Karoutchi, G; Lamont, SG; MacFaul, P; Moss, TA; Pearson, SE; Tonge, M; Walker, GE; Weir, HM; Wilson, Z Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist. J Med Chem 58:8128-40 (2015) [PubMed]  Article 
Target
Name:
Progesterone receptor
Synonyms:
NR3C3 | Nuclear receptor subfamily 3 group C member 3 | PGR | PR | PRGR_HUMAN | progesterone
Type:
Protein
Mol. Mass.:
98979.52
Organism:
Homo sapiens (Human)
Description:
P06401
Residue:
933
Sequence:
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLFPRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLAPSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAAAHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGKPRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTVMDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPDCAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLGPPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPCKAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPPYLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHNYLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPVGVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQLGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAPDLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQFEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRALSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
  
Inhibitor
Name:
BDBM50084948
Synonyms:
CHEMBL195515 | GW7604
Type:
Small organic molecule
Emp. Form.:
C25H22O3
Mol. Mass.:
370.4404
SMILES:
CC\C(=C(/c1ccc(O)cc1)c1ccc(\C=C\C(O)=O)cc1)c1ccccc1
Structure:
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