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

General Information of Drug (ID: DM3AVO1)

Drug Name

DE-081 Drug Info

Synonyms

Apafant; 105219-56-5; WEB-2086; Web 2086; Apafant [USAN:INN]; Apafantum [INN-Latin]; Apafanto [INN-Spanish]; WEB 2086BS; WEB2086; UNII-J613NI05SV; WEB 2086 BS; BRN 4302553; C22H22ClN5O2S; J613NI05SV; CHEMBL280164; NCGC00092377-03; NCGC00092377-02; Apafantum; Apafanto; DSSTox_CID_28900; DSSTox_RID_83168; DSSTox_GSID_48974; 4-(3-(4-(o-Chlorophenyl)-9-methyl-6H-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepin-2-yl)propionyl)morpholine; [3H]apafant; Morpholine; Apafant (ophthalmic formulation), Santen

Indication

Disease Entry	ICD 11	Status	REF
Conjunctivitis	9A60	Discontinued in Phase 2	[1]
Ocular allergy	4A81	Terminated	[2]

Cross-matching ID

PubChem CID: 65889
ChEBI ID: CHEBI:92490
CAS Number: CAS 105219-56-5
TTD Drug ID: DM3AVO1
VARIDT Drug ID: DR01484

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Platelet-activating factor receptor (PTAFR)	TTQL5VC	PTAFR_HUMAN	Modulator	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Discontinued in Phase 2	[4]

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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
Platelet-activating factor receptor (PTAFR)	DTT	PTAFR	6.345	5.947	6.084	6.253
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135

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

Conjunctivitis

ICD Disease Classification

9A60

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Platelet-activating factor receptor (PTAFR)	DTT	PTAFR	3.53E-02	0.33	2.12
P-glycoprotein 1 (ABCB1)	DTP	P-GP	1.64E-01	1.31E-01	1.21E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000113)
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: 1860).
3	Characterization of [3H]apafant binding to PAF receptor on rabbit platelet membranes: a comparison of a microplate filtration system and a standard... J Pharmacol Toxicol Methods. 1996 Sep;36(1):53-62.
4	Altered drug disposition of the platelet activating factor antagonist apafant in mdr1a knockout mice. Eur J Pharm Sci. 2002 Aug;16(3):119-28.