GSK-2881078

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NCATS

Investigational

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C14H13F3N2O2S
Molecular Weight	330.325
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of GSK-2881078

Structure Search

SMILES

C[C@H](CS(C)(=O)=O)N1C=CC2=C1C=CC(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	330.325
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Androgen receptor 42 Target ID: P10275 Gene ID: 367.0 Gene Symbol: AR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/28449232	Modulator 828
Androgen Receptor 167 Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/30825507 \| https://www.ncbi.nlm.nih.gov/pubmed/29982690	Modulator 828		3.99 nM [EC50]

Substance Class	Chemical Created by `admin` on `Sat Dec 16 08:09:30 GMT 2023` Edited by `admin` on `Sat Dec 16 08:09:30 GMT 2023`
Record UNII	47M5ZXU844
Record Status	`Validated (UNII)`
Record Version

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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 Dec 16 08:09:30 GMT 2023 , Edited by admin on Sat Dec 16 08:09:30 GMT 2023

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ChEMBL

CHEMBL3545174

Created by admin on Sat Dec 16 08:09:30 GMT 2023 , Edited by admin on Sat Dec 16 08:09:30 GMT 2023

PRIMARY

CAS

1539314-06-1

Created by admin on Sat Dec 16 08:09:30 GMT 2023 , Edited by admin on Sat Dec 16 08:09:30 GMT 2023

PRIMARY

EPA CompTox

DTXSID701337261

Created by admin on Sat Dec 16 08:09:30 GMT 2023 , Edited by admin on Sat Dec 16 08:09:30 GMT 2023

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MANUFACTURER PRODUCT INFORMATION

GSK-2881078

Created by admin on Sat Dec 16 08:09:30 GMT 2023 , Edited by admin on Sat Dec 16 08:09:30 GMT 2023

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 Dec 16 08:09:30 GMT 2023 , Edited by admin on Sat Dec 16 08:09:30 GMT 2023

PRIMARY

Related Record Type Details


					EJC4C3UYXH

ANDROGEN RECEPTOR

TARGET -> AGONIST

Interaction Type:

ALLOSTERIC

Amount:

Related Record Type Details


					47M5ZXU844

ACTIVE MOIETY

Comments:

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.