Target
Androgen receptor
Ligand
BDBM18699
Substrate
BDBM26258
Meas. Tech.
Competitive Radioligand Displacement Assay and AR-Mediated Transcription Activation Assay
pH
7.4±n/a
Temperature
277.15±n/a K
Ki
0.3±0.12 nM
EC50
500±n/a nM
Comments
Maximal percentage of transcriptional activation observed is 82.9 +/- 14.0 %
Citation
 Dalton, JTMukherjee, AZhu, ZKirkovsky, LMiller, DD Discovery of nonsteroidal androgens. Biochem Biophys Res Commun 244:1-4 (1998) [PubMed]  Article 
Target
Name:
Androgen receptor
Synonyms:
ANDR_RAT | Androgen receptor (AR) | Ar | Estrogen receptor | Nr3c4 | androgen
Type:
Enzyme
Mol. Mass.:
98219.08
Organism:
Rattus norvegicus (Rat)
Description:
P15207
Residue:
902
Sequence:
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREAIQNPGPRHPEAASIAPPGACLQQRQETSPRRRRRQQHPEDGSPQAHIRGTTGYLALEEEQQPSQQQSASEGHPESGCLPEPGAATAPGKGLPQQPPAPPDQDDSAAPSTLSLLGPTFPGLSSCSADIKDILSEAGTMQLLQQQQQQQQQQQQQQQQQQQQQQEVISEGSSSVRAREATGAPSSSKDSYLGGNSTISDSAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYASLLGGPPAVRPTPCAPLAECKGLSLDEGPGKGTEETAEYSSFKGGYAKGLEGESLGCSGSSEAGSSGTLEIPSSLSLYKSGAVDEAAAYQNRDYYNFPLALSGPPHPPPPTHPHARIKLENPSDYGSAWAAAAAQCRYGDLASLHGGSVAGPSTGSPPATASSSWHTLFTAEEGQLYGPGGGGGSSSPSDAGPVAPYGYTRPPQGLASQEGDFSASEVWYPGGVVNRVPYPSPSCVKSEMGPWMENYSGPYGDMRLDSTRDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGENSSAGSPTEDPSQKMTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ
  
Inhibitor
Name:
BDBM18699
Synonyms:
(2R)-3-bromo-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide | CHEMBL296323 | R-3
Type:
Small organic molecule
Emp. Form.:
C11H10BrF3N2O4
Mol. Mass.:
371.107
SMILES:
C[C@](O)(CBr)C(=O)Nc1ccc(c(c1)C(F)(F)F)[N+]([O-])=O |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM26258
Synonyms:
(1S,2R,9R,10R,11S,14S,15S)-14-hydroxy-9,14,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one | [3H]MIB | [3H]Mibolerone
Type:
radiolabeled ligand
Emp. Form.:
C20H30O2
Mol. Mass.:
302.451
SMILES:
[H][C@@]12CC[C@](C)(O)[C@@]1(C)CC[C@]1([H])[C@@]3([H])CCC(=O)C=C3C[C@@H](C)[C@@]21[H] |c:20|
Structure:
Search PDB for entries with ligand similarity: