BDBM50094975 956104-40-8::ARN-509::JNJ-56021927::US10053433, ARN-509::apalutamide

SMILES CNC(=O)c1ccc(cc1F)N1C(=S)N(C(=O)C11CCC1)c1cnc(C#N)c(c1)C(F)(F)F

InChI Key InChIKey=HJBWBFZLDZWPHF-UHFFFAOYSA-N

Data  5 KI  9 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 14 hits for monomerid = 50094975   

TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 3.28E+3nMpH: 7.5Assay Description:Briefly, the AR LBD is expressed as a fusion with the Gal4 transcription factor, which binds to the Gal4 reporter DNA. Upon activation with agonist h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2018
Entry Details
Go to US Patent

TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 1.95E+4nMpH: 7.5Assay Description:An AR-response element is contained within the mmTV sequence and drives the expression of luciferase. The effect of antiandrogens (competitive antago...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2018
Entry Details
Go to US Patent

TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 3.11E+3nMpH: 7.5Assay Description:Briefly, the AR LBD is expressed as a fusion with the Gal4 transcription factor, which binds to the Gal4 reporter DNA. Upon activation with agonist h...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2018
Entry Details
Go to US Patent

TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 15nMAssay Description:Displacement of [3H]-R1881 from AR in human LNCaP cells preincubated for 30 mins followed by [3H]-R1881 addition measured after 30 mins by microbeta ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2019
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 16nMAssay Description:Displacement of [3H]-R1881 from AR in human LNCaP cells preincubated for 30 mins followed by [3H]-R1881 addition measured after 30 mins by microbeta ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2019
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 16nMAssay Description:Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 16nMAssay Description:Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 160nMAssay Description:Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataIC50: 200nMAssay Description:Inhibition of androgen receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataKi:  35nMAssay Description:Antagonist activity at androgen receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2016
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataKi:  93nMAssay Description:Inhibition of androgen receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataKi:  1.45E+3nMAssay Description:Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
University of California

US Patent
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataKi:  1.45E+3nMAssay Description:Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetAndrogen receptor(Rat)
University of Tennessee Health Science Center

Curated by ChEMBL
LigandPNGBDBM50094975(US10053433, ARN-509 | ARN-509 | JNJ-56021927 | apa...)
Affinity DataKi:  1.45E+3nMAssay Description:Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed