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

General Information of Drug (ID: DMMXR3L)

Drug Name

PMX205 Drug Info

Synonyms

PMX 205; 514814-49-4; PMX-205; UNII-DC25O3L7KZ; Hydrocinnamate-(orn-Pro-dcha-Trp-Arg); DC25O3L7KZ; Cyclic hexapeptide complement C5a antagonist; N-[(3S,9S,12S,15R,18S)-15-(cyclohexylmethyl)-9-[3-(diaminomethylideneamino)propyl]-12-(1H-indol-3-ylmethyl)-2,8,11,14,17-pentaoxo-1,7,10,13,16-pentazabicyclo[16.3.0]henicosan-3-yl]-3-phenylpropanamide; HC-[OP(D-Cha)WR]; SCHEMBL12971708; CHEBI:144869; LP-16; ZINC95627847; HY-110136; CS-0032991; A16946; hydrocinnamate-cyclo(ornithyl-prolyl-D-cyclohexylalanyl-tryptophyl-arginyl); (5->1)-lactam-N(2)-(1-oxo-3-phenylpropyl)-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-L-arginine; N-[(3R,6S,9S,15S,20aS)-9-(3-carbamimidamidopropyl)-3-(cyclohexylmethyl)-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl]-3-phenylpropanamide

Indication

Disease Entry	ICD 11	Status	REF
Central nervous system disease	8A04-8D87	Preclinical	[1]

Cross-matching ID

PubChem CID: 6918845
ChEBI ID: CHEBI:144869
CAS Number: CAS 514814-49-4
TTD Drug ID: DMMXR3L

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting C5a anaphylatoxin chemotactic receptor (C5AR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Avacopan	DM5LQHB	Anca-associated vasculitis	4A44.A	Approved	[3]
PMX-53	DMZUAJ4	Atopic dermatitis	EA80	Phase 2	[4]
NN8209	DM2TDE7	Rheumatoid arthritis	FA20	Discontinued in Phase 2	[5]
NN8210	DM8Z5VH	Rheumatoid arthritis	FA20	Discontinued in Phase 1	[5]
RPR121154	DM9DXHM	Discovery agent	N.A.	Investigative	[6]
W54011	DMQI7BA	Discovery agent	N.A.	Investigative	[7]
C5aR pepducins	DMEK4HZ	Inflammation	1A00-CA43.1	Investigative	[6]
NDT9520492	DMFKX7Z	Discovery agent	N.A.	Investigative	[8]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
C5a anaphylatoxin chemotactic receptor (C5AR1)	TTHXFA1	C5AR1_HUMAN	Antagonist	[2]

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References

1	Preclinical Pharmacokinetics of Complement C5a Receptor Antagonists PMX53 and PMX205 in Mice. ACS Omega. 2020 Jan 30;5(5):2345-2354.
2	Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Sci Rep. 2018 May 25;8(1):8101.
3	Clinical pipeline report, company report or official report of ChemoCentryx.
4	Company report (Arana Therapeutics)
5	Complement in immune and inflammatory disorders: therapeutic interventions. J Immunol. 2013 Apr 15;190(8):3839-47.
6	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: 32).
7	Identification of a potent and orally active non-peptide C5a receptor antagonist. J Biol Chem. 2002 Dec 20;277(51):49403-7.
8	Molecular characterization of the gerbil C5a receptor and identification of a transmembrane domain V amino acid that is crucial for small molecule ... J Biol Chem. 2005 Dec 9;280(49):40617-23.