Target
Androgen receptor
Ligand
BDBM18578
Substrate
BDBM18161
Meas. Tech.
AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay
pH
7.4±n/a
Temperature
310.15±n/a K
Ki
0.5±n/a nM
EC50
0.4±0.1 nM
Comments
hAR agonist efficacy = 74 +/- 7 %
Citation
 van Oeveren, AMotamedi, MMartinborough, EZhao, SShen, YWest, SChang, WKallel, AMarschke, KBLópez, FJNegro-Vilar, AZhi, L Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. Bioorg Med Chem Lett 17:1527-31 (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:
BDBM18578
Synonyms:
6-[bis(2,2-difluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | 6-bisalkylamino-2-quinolinone, 6c
Type:
Small organic molecule
Emp. Form.:
C14H11F7N2O
Mol. Mass.:
356.2388
SMILES:
FC(F)CN(CC(F)F)c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM18161
Synonyms:
(1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-5-one | (5alpha,17beta)-17-hydroxyandrostan-3-one | CHEMBL27769 | DHT | Dihydrotestosterone | [3H]DHT
Type:
Steroid
Emp. Form.:
C19H30O2
Mol. Mass.:
290.4403
SMILES:
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])CC(=O)CC[C@]12C |r|
Structure:
Search PDB for entries with ligand similarity: