Target
Estrogen receptor beta
Ligand
BDBM19459
Substrate
BDBM17289
Meas. Tech.
Competition-Based Ligand Binding Assay and Transactivation Assay.
IC50
61±n/a nM
EC50
73±n/a nM
Citation
 Güngör, TChen, YGolla, RMa, ZCorte, JRNorthrop, JPBin, BDickson, JKStouch, TZhou, RJohnson, SESeethala, RFeyen, JH Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators. J Med Chem 49:2440-55 (2006) [PubMed]  Article 
Target
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:
MDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPSNVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVNRETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGHNDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLHCAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTKLADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDLVLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDADSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMKCKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ
  
Inhibitor
Name:
BDBM19459
Synonyms:
5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one | CHEMBL44 | Genistein | Genistein, 8 | Genisteol | Prunetol | US8552057, 2 | cid_5280961
Type:
Phytoestrogen
Emp. Form.:
C15H10O5
Mol. Mass.:
270.2369
SMILES:
Oc1ccc(cc1)-c1coc2cc(O)cc(O)c2c1=O
Structure:
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Substrate
Name:
BDBM17289
Synonyms:
(1S,10R,11S,15S)-5-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2,4,6-trien-14-one | CHEMBL1405 | Estrone | Estrone (E1) | Estrone, 15 | Estrovarin | Kestrone | Theelin | Unigen | [2,4,6,7-3H]-E1 | [2,4,6,7-3H]-Estrone | folliculin
Type:
Steroid
Emp. Form.:
C18H22O2
Mol. Mass.:
270.3661
SMILES:
[H][C@@]12CCC(=O)[C@@]1(C)CC[C@]1([H])c3ccc(O)cc3CC[C@@]21[H]
Structure:
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