6IAR

Tricyclic indazoles a novel class of selective estrogen receptor degrader antagonists

Summary for 6IAR

Entry DOI	10.2210/pdb6iar/pdb
Descriptor	Estrogen receptor, 3-[4-[(6~{R})-7-(2-methylpropyl)-3,6,8,9-tetrahydropyrazolo[4,3-f]isoquinolin-6-yl]phenyl]propanoic acid (3 entities in total)
Functional Keywords	nuclear hormone receptor inhibitor downregulation estrogen receptor modulators, dna binding protein
Biological source	Homo sapiens (Human)
Total number of polymer chains	1
Total formula weight	27470.29
Authors	Scott, J.S.,Bailey, A.,Buttar, D.,Carbajo, R.J.,Curwen, J.,Davies, R.D.M.,Degorce, S.L.,Donald, C.,Gangl, E.,Greenwood, R.,Groombridge, S.D.,Johnson, T.,Lamont, S.,Lawson, M.,Lister, A.,Morrow, C.,Moss, T.,Pink, J.H.,Polanski, R. (deposition date: 2018-11-27, release date: 2019-01-23, Last modification date: 2019-04-24)
Primary citation	Scott, J.S.,Bailey, A.,Buttar, D.,Carbajo, R.J.,Curwen, J.,Davey, P.R.J.,Davies, R.D.M.,Degorce, S.L.,Donald, C.,Gangl, E.,Greenwood, R.,Groombridge, S.D.,Johnson, T.,Lamont, S.,Lawson, M.,Lister, A.,Morrow, C.J.,Moss, T.A.,Pink, J.H.,Polanski, R. Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists. J.Med.Chem., 62:1593-1608, 2019 Cited by PubMed: 30640465 DOI: 10.1021/acs.jmedchem.8b01837 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.84 Å)

Structure validation