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Target
Estrogen receptor
Ligand
BDBM368203
Substrate
n/a
Meas. Tech.
ChEMBL_1833831 (CHEMBL4333839)
IC50
0.100000±n/a nM
Citation
 Kahraman, M; Govek, SP; Nagasawa, JY; Lai, A; Bonnefous, C; Douglas, K; Sensintaffar, J; Liu, N; Lee, K; Aparicio, A; Kaufman, J; Qian, J; Shao, G; Prudente, R; Joseph, JD; Darimont, B; Brigham, D; Heyman, R; Rix, PJ; Hager, JH; Smith, ND Maximizing ER-? Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927. ACS Med Chem Lett 10:50-55 (2019) [PubMed]  Article 
Target
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:
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLLLEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
  
Inhibitor
Name:
BDBM368203
Synonyms:
US10227334, Example (S)-3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1- yl)propoxy)phenyl)-2H-chromen-6-ol
Type:
Small organic molecule
Emp. Form.:
C30H33NO4
Mol. Mass.:
471.5873
SMILES:
C[C@@H](COc1ccc(cc1)[C@@H]1Oc2ccc(O)cc2C(C)=C1c1cccc(O)c1)N1CC[C@@H](C)C1 |c:22|
Structure:
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