Reaction Details Report a problem with these data
Target
Progesterone receptor
Ligand
BDBM20608
Substrate
n/a
Meas. Tech.
ChEMBL_1519263 (CHEMBL3624760)
IC50
<100000±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:
BDBM20608
Synonyms:
4-Hydroxytamoxifen | 4-Hydroxytamoxifen (9) | 4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl]phenol | AFIMOXIFENE | CHEMBL489 | [3H]4-OHT | cid_449459
Type:
Small organic molecule
Emp. Form.:
C26H29NO2
Mol. Mass.:
387.514
SMILES:
CC\C(=C(/c1ccc(O)cc1)c1ccc(OCCN(C)C)cc1)c1ccccc1
Structure:
Search PDB for entries with ligand similarity: