Reaction Details |
| Report a problem with these data |
Target | Estrogen receptor beta |
---|
Ligand | BDBM19442 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1497879 (CHEMBL3582786) |
---|
IC50 | 240±n/a nM |
---|
Citation | Lai, A; Kahraman, M; Govek, S; Nagasawa, J; Bonnefous, C; Julien, J; Douglas, K; Sensintaffar, J; Lu, N; Lee, KJ; Aparicio, A; Kaufman, J; Qian, J; Shao, G; Prudente, R; Moon, MJ; Joseph, JD; Darimont, B; Brigham, D; Grillot, K; Heyman, R; Rix, PJ; Hager, JH; Smith, 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 beta |
---|
Name: | Estrogen receptor beta |
Synonyms: | ER-beta | ESR2 | ESR2_HUMAN | ESTRB | Estradiol receptor beta (ERβ) | Estrogen receptor | Estrogen receptor (ER beta) | Estrogen receptor beta | Estrogen receptor beta (ER beta) | Estrogen receptor beta (ER) | NR3A2 | Nuclear receptor subfamily 3 group A member 2 | estrogen beta |
Type: | Protein |
Mol. Mass.: | 59238.43 |
Organism: | Homo sapiens (Human) |
Description: | Q92731 |
Residue: | 530 |
Sequence: | MDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPS
NVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVN
RETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGH
NDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLH
CAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTK
LADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDL
VLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDA
DSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMK
CKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ
|
|
|
BDBM19442 |
---|
n/a |
---|
Name | BDBM19442 |
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 |
Type | Small organic molecule |
Emp. Form. | C28H29NO4S |
Mol. Mass. | 475.599 |
SMILES | COc1ccc(cc1)-c1sc2cc(O)ccc2c1Oc1ccc(OCCN2CCCCC2)cc1 |
Structure |
|