Details of the Drug

General Information of Drug (ID: DMIX891)

Drug Name

GSK2292767

Synonyms

GSK2292767; 1254036-66-2; GSK-2292767; 4M4E8NZ73C; Methanesulfonamide, N-[5-[4-[5-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]-, rel-; CHEMBL4434674; PI3Kdelta inhibitor GS2292767; n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide; N-(5-(4-(5-(((2R,6S)-2,6-Dimethylmorpholino)methyl)oxazol-2-yl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide; Methanesulfonamide, N-(5-(4-(5-(((2R,6S)-2,6-dimethyl-4-morpholinyl)methyl)-2-oxazolyl)-1H-indazol-6-yl)-2-methoxy-3-pyridinyl)-, rel-; N-[5-[4-[5-[[(2S,6R)-2,6-Dimethylmorpholin-4-yl]methyl]-1,3-oxazol-2-yl]-1H-indazol-6-yl]-2-methoxypyridin-3-yl]methanesulfonamide; UNII-4M4E8NZ73C; SCHEMBL173490; C24H28N6O5S; GTPL10633; EX-A994; BCP24323; BDBM50521218; MFCD22572737; s7938; AKOS032945160; CCG-269791; compound 2 [PMID: 30532965]; compound 3 [PMID: 26301626]; AC-32649; HY-15280; CS-0003832; Q27464135; N-{5-[4-(5-{[(2R,6S)-2,6-dimethylmorpholin-4-yl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-methoxypyridin-3-yl}methanesulfonamide; rel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Phase 1	[1]
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Drug Type

Small molecule

Structure

3D MOL

2D MOL

Chemical Identifiers

Formula: C24H28N6O5S
Canonical SMILES: CC1CN(CC(O1)C)CC2=CN=C(O2)C3=C4C=NNC4=CC(=C3)C5=CC(=C(N=C5)OC)NS(=O)(=O)C
InChI: InChI=1S/C24H28N6O5S/c1-14-11-30(12-15(2)34-14)13-18-9-26-23(35-18)19-5-16(6-21-20(19)10-27-28-21)17-7-22(29-36(4,31)32)24(33-3)25-8-17/h5-10,14-15,29H,11-13H2,1-4H3,(H,27,28)/t14-,15+
InChIKey: NLUPPCTVKHDVIQ-GASCZTMLSA-N

Cross-matching ID

PubChem CID: 49783923
TTD ID: DDE6F1

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase delta (PIK3CD)	TTGBPJE	PK3CD_HUMAN	Inhibitor	[2]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease

Asthma

ICD Disease Classification

CA23

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
PI3-kinase delta (PIK3CD)	DTT	PIK3CD	4.31E-16	-0.37	-0.91

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This Drug

References

1	ClinicalTrials.gov (NCT03045887) A Single-centre, Double-blind (Sponsor Open), Placebo Controlled Two Part Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Single and Repeat Doses of GSK2292767 as a Dry Powder in Healthy Participants Who Smoke Cigarettes. U.S.National Institutes of Health.
2	Translation of Inhaled Drug Optimization Strategies into Clinical Pharmacokinetics and Pharmacodynamics Using GSK2292767A, a Novel Inhaled Phosphoinositide 3-Kinase delta Inhibitor. J Pharmacol Exp Ther. 2019 Jun;369(3):443-453.