Drug Information

Drug General Information
Drug ID
D02QQB
Former ID
DIB002099
Drug Name
A-216546
Synonyms
ABT-546; (2S,3R,4S)-1-[2-(Dibutylamino)-2-oxoethyl]-2-(2,2-dimethylpentyl)-4-(7-methoxy-1,3-benzodioxol-5-yl)tetrahydro-1H-pyrrole-3-carboxylic acid
Indication Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48] Discontinued in Phase 1 [546860]
CAS Number
CAS 195707-49-4
Target and Pathway
Target(s) Endothelin-1 receptor Target Info Antagonist [525441], [551871]
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
Renin secretion
Pathways in cancer
NetPath Pathway IL4 Signaling Pathway
PANTHER Pathway Endothelin signaling pathway
Pathway Interaction Database Endothelins
EGFR-dependent Endothelin signaling events
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways Prostaglandin Synthesis and Regulation
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 546860Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010699)
Ref 525441Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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