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Target
Progesterone receptor
Ligand
BDBM50144438
Substrate
n/a
Meas. Tech.
ChEMBL_474423 (CHEMBL934256)
IC50
4.9±n/a nM
Citation
Fensome, A; Adams, WR; Adams, AL; Berrodin, TJ; Cohen, J; Huselton, C; Illenberger, A; Kern, JC; Hudak, VA; Marella, MA; Melenski, EG; McComas, CC; Mugford, CA; Slayden, OD; Yudt, M; Zhang, Z; Zhang, P; Zhu, Y; Winneker, RC; Wrobel, JE Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348). J Med Chem 51:1861-73 (2008) [PubMed] Article
More Info.:
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:
Human
Description:
P06401
Residue:
933
Sequence:
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLFPRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLAPSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAAAHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGKPRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTVMDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPDCAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLGPPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPCKAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPPYLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHNYLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPVGVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQLGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAPDLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQFEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRALSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
Inhibitor
Name:
BDBM50144438
Synonyms:
5-(4,4-Dimethyl-2-oxo-1,4-dihydro-2H-benzo[d][1,3]oxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile | 5-(4,4-dimethyl-2-oxo-2,4-dihydro-1H-benzo[d][1,3]oxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile | CHEMBL67860
Type:
Small organic molecule
Emp. Form.:
C16H15N3O2
Mol. Mass.:
281.3092
SMILES:
Cn1c(ccc1-c1ccc2NC(=O)OC(C)(C)c2c1)C#N