Reaction Details |
| Report a problem with these data |
Target | Androgen receptor |
---|
Ligand | BDBM18524 |
---|
Substrate/Competitor | 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 | 4.6±n/a nM |
---|
EC50 | 0.2±0.02 nM |
---|
Comments | Agonist efficacy is 95 +/- 2 %.With I.V. dosing, the half-life was 1.7 h. Oral dosing at 10 mg/kg resulted in an AUC of 3.15 ug.h/mL with oral bioavailability of 43%. |
---|
Citation | Martinborough, E; Shen, Y; Oeveren, A; Long, YO; Lau, TL; Marschke, KB; Chang, WY; López, FJ; Vajda, EG; Rix, PJ; Viveros, OH; Negro-Vilar, A; Zhi, L Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators. J Med Chem50:5049-52 (2007) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Androgen receptor |
---|
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: | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
|
|
|
BDBM18524 |
---|
BDBM18161 |
---|
Name | BDBM18524 |
Synonyms: | 6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | CHEMBL436784 | LGD2226 |
Type | Small organic molecule |
Emp. Form. | C14H9F9N2O |
Mol. Mass. | 392.2197 |
SMILES | FC(F)(F)CN(CC(F)(F)F)c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F |
Structure |
|