Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMMCYZ8)

Drug Name

PQR309 Drug Info

Synonyms

Bimiralisib; PQR309; 1225037-39-7; PI3K-IN-2; PQR-309; UNII-6Z3QHB00LB; 6Z3QHB00LB; 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; 5-[bis(morpholin-4-yl)-1,3,5-triazin-2-yl]-4-(trifluoromethyl)pyridin-2-amine; 5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; Bimiralisib [INN]; Bimiralisib [USAN]; PQR309; Bimiralisib; Bimiralisib [WHO-DD]; NCB5; SCHEMBL1309049; GTPL8383; PQR309; Bimiralisib free base; ADGGYDAFIHSYFI-UHFFFAOYSA-N; EX-A2018; BCP15887; PQR-309(PI3K-IN-2)

Indication

Disease Entry	ICD 11	Status	REF
Squamous head and neck cell carcinom	2D60.0	Phase 2	[1]
Pain	MG30-MG3Z	Phase 1	[2]

Cross-matching ID

PubChem CID: 58507717
CAS Number: CAS 1225037-39-7
TTD Drug ID: DMMCYZ8

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase beta (PIK3CB)	TTTHBCA	PK3CB_HUMAN	Inhibitor	[3]
PI3-kinase gamma (PIK3CG)	TTHBTOP	PK3CG_HUMAN	Inhibitor	[4]
Serine/threonine-protein kinase mTOR (mTOR)	TTCJG29	MTOR_HUMAN	Inhibitor	[5]

------------------------------------------------------------------------------------

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
PI3-kinase beta (PIK3CB)	DTT	PIK3CB	5.331	6.074	6.017	5.702
Serine/threonine-protein kinase mTOR (mTOR)	DTT	MTOR	5.425	4.35	5.106	5.188

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Squamous head and neck cell carcinom

ICD Disease Classification

2D60.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
PI3-kinase gamma (PIK3CG)	DTT	PIK3CG	1.98E-01	-0.05	-0.55

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	ClinicalTrials.gov (NCT03740100) Single-arm Study With Bimiralisib in Patients With HNSCC Harboring NOTCH1 Loss of Function Mutations (HNSCC). U.S. National Institutes of Health.
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8383).
3	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2154).
4	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2155).
5	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2109).