Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM18175 |
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Substrate/Competitor | BDBM18161 |
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Meas. Tech. | Receptor Binding and Transactivation Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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Ki | 2.2±n/a nM |
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EC50 | 20±n/a nM |
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Comments | Compound is full agonist with IA>85% relative to DHT control (IA=100%) |
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Citation | Li, JJ; Sutton, JC; Nirschl, A; Zou, Y; Wang, H; Sun, C; Pi, Z; Johnson, R; Krystek, SR; Seethala, R; Golla, R; Sleph, PG; Beehler, BC; Grover, GJ; Fura, A; Vyas, VP; Li, CY; Gougoutas, JZ; Galella, MA; Zahler, R; Ostrowski, J; Hamann, LG Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications. J Med Chem50:3015-3025 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Androgen receptor |
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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.
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Residue: | 920 |
Sequence: | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
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BDBM18175 |
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BDBM18161 |
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Name | BDBM18175 |
Synonyms: | 4-[(3aR,4R,6aS)-4-hydroxy-1-oxo-octahydrocyclopenta[c]pyrrol-2-yl]-2-chloro-3-methylbenzonitrile | Pyrrolidin-2-one, 9 |
Type | Small organic molecule |
Emp. Form. | C15H15ClN2O2 |
Mol. Mass. | 290.745 |
SMILES | [H][C@]12CN(C(=O)[C@@]1([H])CC[C@H]2O)c1ccc(C#N)c(Cl)c1C |r| |
Structure |
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