Target
Androgen receptor
Ligand
BDBM18617
Substrate
BDBM8885
Meas. Tech.
Competitive Ligand Binding Assay, GR-Mediated Agonist Activity Assay, and IL-6 Repression Assay
Ki
150±n/a nM
Citation
 Hudson, ARRoach, SLHiguchi, RIPhillips, DPBissonnette, RPLamph, WWYen, JLi, YAdams, MEValdez, LJVassar, ACuervo, CKallel, EAGharbaoui, CJMais, DEMiner, JNMarschke, KBRungta, DNegro-Vilar, AZhi, L Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma. J Med Chem 50:4699-709 (2007) [PubMed]  Article 
Target
Name:
Androgen receptor
Synonyms:
ANDR_HUMAN | AR | Androgen Receptor | Androgen receptor (AR) | Androgen receptor/Baculoviral IAP repeat-containing protein 2 | DHTR | Dihydrotestosterone receptor | NR3C4 | Nuclear receptor subfamily 3 group C member 4
Type:
Receptor
Mol. Mass.:
99185.27
Organism:
Homo sapiens (Human)
Description:
CHO cells were stably transfected with human AR gene.
Residue:
920
Sequence:
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQSRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAAGPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAPYGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRLETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKLTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ
  
Inhibitor
Name:
BDBM18617
Synonyms:
(18Z)-12-methoxy-18-{[3-(methoxymethyl)thiophen-2-yl]methylidene}-3,5,5-trimethyl-17-oxa-6-azatetracyclo[8.8.0.0^{2,7}.0^{11,16}]octadeca-1(10),2(7),3,8,11,13,15-heptaen-13-ol | Methyl ether, 9
Type:
Small organic molecule
Emp. Form.:
C27H27NO4S
Mol. Mass.:
461.573
SMILES:
COCc1ccsc1\C=C1/Oc2ccc(O)c(OC)c2-c2ccc3NC(C)(C)C=C(C)c3c12 |t:30|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM8885
Synonyms:
(1S,2R,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one | 17beta-Hydroxyandrost-4-en-3-one | Testosterone | Testosterone, 1 | US9682960, Testosterone
Type:
Steroid
Emp. Form.:
C19H28O2
Mol. Mass.:
288.4244
SMILES:
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C |r,t:18|
Structure:
Search PDB for entries with ligand similarity: