Reaction Details |
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Target | Estrogen receptor beta |
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Ligand | BDBM19968 |
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Substrate/Competitor | 17beta-estradiol (E2) |
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Meas. Tech. | Estrogen Receptor Binding Assay and Cell-Based Transcriptional Assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 0.19±0.01 nM |
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EC50 | 0.66±0.04 nM |
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Comments | Efficacy=101% |
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Citation | Norman, BH; Dodge, JA; Richardson, TI; Borromeo, PS; Lugar, CW; Jones, SA; Chen, K; Wang, Y; Durst, GL; Barr, RJ; Montrose-Rafizadeh, C; Osborne, HE; Amos, RM; Guo, S; Boodhoo, A; Krishnan, V Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. J Med Chem49:6155-7 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Estrogen receptor beta |
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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
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BDBM19968 |
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17beta-estradiol (E2) |
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Name | BDBM19968 |
Synonyms: | (2R,6S,7R)-7-(4-hydroxyphenyl)-8-oxatricyclo[7.4.0.0^{2,6}]trideca-1(13),9,11-trien-12-ol | (2R,6S,7R)-7-(4-hydroxyphenyl)-8-oxatricyclo[7.4.0.0^{2,6}]trideca-1(9),10,12-trien-12-ol | Benzopyran derivative., 4b(racemate) | SERBA-1 | racemic mixture |
Type | Small organic molecule |
Emp. Form. | C18H18O3 |
Mol. Mass. | 282.3337 |
SMILES | Oc1ccc(cc1)[C@@H]1Oc2ccc(O)cc2[C@@H]2CCC[C@H]12 |r| |
Structure |
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