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

General Information of Drug (ID: DMML7BE)

Drug Name

XL147 Drug Info

Synonyms

N-[3-(2,1,3-Benzothiadiazol-5-ylamino)quinoxalin-2-yl]-4-methylbenzenesulfonamide; 956958-53-5; XL147 analogue; PI3K inhibitor X; XL 147; Pilaralisib analogue; N-[3-(2,1,3-benzothiadiazol-5-ylamino)quinoxalin-2-yl]-4-methylbenzenesulfonamide; N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide; CHEBI:71957; C21H16N6O2S2; N-(3-(benzo[c][1,2,5]thiadiazol-5-ylamino)quinoxalin-2-yl)-4-methylbenzenesulfonamide; Benzenesulfonamide, N-[3-(2,1,3-benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methyl-; 1033110-57-4; PubChem22457; XL-147 derivative 2; cc-43; AC1Q2LO8; AC1LZ6F0; SAR245408 + MSC1936369B

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 2	[1]

Therapeutic Class

Anticancer Agents

Cross-matching ID

PubChem CID: 1893730
ChEBI ID: CHEBI:71957
CAS Number: CAS 1033110-57-4
TTD Drug ID: DMML7BE
INTEDE Drug ID: DR1854

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase gamma (PIK3CG)	TTHBTOP	PK3CG_HUMAN	Modulator	[2]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Aldehyde oxidase (AOX1)	DEAWHS8	AOXA_HUMAN	Phase 2	[3]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Aldehyde oxidase (AOX1)	DME	AOX1	10.746	6.359	9.496	4.508

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

Solid tumour/cancer

ICD Disease Classification

2A00-2F9Z

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
Aldehyde oxidase (AOX1)	DME	AOX1	3.41E-01	-1.75E-01	-8.17E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	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: 7963).
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. (Target id: 2156).
3	Characterization of aldehyde oxidase enzyme activity in cryopreserved human hepatocytes. Drug Metab Dispos. 2012 Feb;40(2):267-75.