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TargetEstrogen receptor
LigandBDBM19442
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1497878 (CHEMBL3582785)
IC50 42±n/a nM
Citation Lai, AKahraman, MGovek, SNagasawa, JBonnefous, CJulien, JDouglas, KSensintaffar, JLu, NLee, KJAparicio, AKaufman, JQian, JShao, GPrudente, RMoon, MJJoseph, JDDarimont, BBrigham, DGrillot, KHeyman, RRix, PJHager, JHSmith, ND Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem58:4888-904 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Estrogen receptor
Name:Estrogen receptor
Synonyms:ER | ER-alpha | ESR | ESR1 | ESR1_HUMAN | Estradiol receptor | Estrogen receptor | Estrogen receptor (ER alpha) | Estrogen receptor (ER-alpha) | Estrogen receptor alpha (ER alpha) | Estrogen receptor alpha (ER) | NR3A1 | Nuclear receptor subfamily 3 group A member 1
Type:Protein
Mol. Mass.:66230.44
Organism:Homo sapiens (Human)
Description:P03372
Residue:595
Sequence:
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
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  Blast E-value cutoff:
BDBM19442
n/a
NameBDBM19442
Synonyms:2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol | 2-(4-methoxyphenyl)-3-{4-[2-(piperidin-1-yl)ethoxy]phenoxy}-1-benzothiophen-6-ol | Arzoxifene
TypeSmall organic molecule
Emp. Form.C28H29NO4S
Mol. Mass.475.599
SMILESCOc1ccc(cc1)-c1sc2cc(O)ccc2c1Oc1ccc(OCCN2CCCCC2)cc1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: