Reaction Details |
| Report a problem with these data |
Target | Estrogen receptor |
---|
Ligand | BDBM50180684 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1674627 (CHEMBL4024656) |
---|
IC50 | 10±n/a nM |
---|
Citation | Tria, GS; Abrams, T; Baird, J; Burks, HE; Firestone, B; Gaither, LA; Hamann, LG; He, G; Kirby, CA; Kim, S; Lombardo, F; Macchi, KJ; McDonnell, DP; Mishina, Y; Norris, JD; Nunez, J; Springer, C; Sun, Y; Thomsen, NM; Wang, C; Wang, J; Yu, B; Tiong-Yip, CL; Peukert, S Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem61:2837-2864 (2018) [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
|
|
|
BDBM50180684 |
---|
n/a |
---|
Name | BDBM50180684 |
Synonyms: | 4-OHT | Afimoxifene | TamoGel |
Type | Small organic molecule |
Emp. Form. | C26H29NO2 |
Mol. Mass. | 387.514 |
SMILES | CC\C(=C(/c1ccccc1)c1ccc(OCCN(C)C)cc1)c1ccc(O)cc1 |
Structure |
|