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Details

Stereochemistry ABSOLUTE
Molecular Formula C14H13F3N2O2S
Molecular Weight 330.327
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GSK-2881078

SMILES

C[C@]([H])(CS(=O)(=O)C)n1ccc2c1ccc(C#N)c2C(F)(F)F

InChI

InChIKey=SKDVMPZQJMZEAC-SECBINFHSA-N
InChI=1S/C14H13F3N2O2S/c1-9(8-22(2,20)21)19-6-5-11-12(19)4-3-10(7-18)13(11)14(15,16)17/h3-6,9H,8H2,1-2H3/t9-/m1/s1

HIDE SMILES / InChI

Molecular Formula C14H13F3N2O2S
Molecular Weight 330.327
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P10275
Gene ID: 367.0
Gene Symbol: AR
Target Organism: Homo sapiens (Human)
3.99 nM [EC50]
Substance Class Chemical
Created
by admin
on Sat Jun 26 03:21:59 UTC 2021
Edited
by admin
on Sat Jun 26 03:21:59 UTC 2021
Record UNII
47M5ZXU844
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GSK-2881078
Code English
2881078
Code English
1H-INDOLE-5-CARBONITRILE, 1-((1R)-1-METHYL-2-(METHYLSULFONYL)ETHYL)-4-(TRIFLUOROMETHYL)-
Systematic Name English
(R)-1-(1-(METHYLSULFONYL)PROPAN-2-YL)-4-(TRIFLUOROMETHYL)-1H-INDOLE-5-CARBONITRILE
Systematic Name English
Code System Code Type Description
FDA UNII
47M5ZXU844
Created by admin on Sat Jun 26 03:21:59 UTC 2021 , Edited by admin on Sat Jun 26 03:21:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL3545174
Created by admin on Sat Jun 26 03:21:59 UTC 2021 , Edited by admin on Sat Jun 26 03:21:59 UTC 2021
PRIMARY
CAS
1539314-06-1
Created by admin on Sat Jun 26 03:21:59 UTC 2021 , Edited by admin on Sat Jun 26 03:21:59 UTC 2021
PRIMARY
MANUFACTURER PRODUCT INFORMATION
GSK-2881078
Created by admin on Sat Jun 26 03:21:59 UTC 2021 , Edited by admin on Sat Jun 26 03:21:59 UTC 2021
PRIMARY MedKoo CAT NO.: 526708, CAS NO.: 1539314-06-1Description: GSK-2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia. GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. (last updated: 6/24/2016).
PUBCHEM
86709174
Created by admin on Sat Jun 26 03:21:59 UTC 2021 , Edited by admin on Sat Jun 26 03:21:59 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> AGONIST
SARMs bind to the androgen receptor and induce conformational changes that facilitate interactions with specific co-activator and co-repressor proteins. These interactions result in downstream regulation of target genes and other receptor-mediated pathway. Induction of anabolic effects on muscle and bone, overall body metabolism and physical function could be useful for many clinical conditions in which subjects experience muscle wasting and impaired physical function.
ALLOSTERIC
Related Record Type Details
ACTIVE MOIETY
Official Title: A Randomized Double-blind (Sponsor Unblind) Placebo Controlled Study in Healthy Subjects to Evaluate: Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Repeat Doses of GSK2881078, the Selective Androgen Receptor Modulator With an Open Label Dosing Arm to Evaluate the Effect of CYP3A4 Inhibition on Pharmacokinetics of GSK2881078 Purpose: GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. Part A of this study will evaluate the safety, efficacy and pharmacokinetics of GSK2881078 in healthy, older men and post-menopausal women who will take daily dosing for 28 days and be followed for a total of 70 days. Part B of this study will characterize the effect of Cytochrome P450 3A4 (CYP3A4) inhibition on the GSK2881078 pharmacokinetics. Part B will only be conducted if safe and efficacious dose is identified in Part A. Part A will include healthy older males and post-menopausal females, and randomize approximately 60 subjects (about 15 per cohort (4 cohorts)) to complete approximately 48 (about 12 per cohort). Part B will enroll one cohort of approximately 15 healthy male subjects to complete approximately 12. The study duration will be approximately 115 days for Part A and 122 days for Part B.