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

General Information of Drug (ID: DM4UN9A)

• Drug Name: ABT-839 Drug Info
• Synonyms: ABT-839; CHEMBL29982; 216234-25-2; 2-{(5-{[BUTYL-(2-CYCLOHEXYL-ETHYL)-AMINO]-METHYL}-2'-METHYL-BIPHENYL-2-CARBONYL)-AMINO]-4-METHYLSULFANYL-BUTYRIC ACID; A 228839; AC1L9KPG; SCHEMBL629301; BDBM17325; 1n94; ZINC3973581; KB-74366; (2S)-2-[(4-{[butyl(2-cyclohexylethyl)amino]methyl}-2-(2-methylphenyl)phenyl)formamido]-4-(methylsulfanyl)butanoic acid; N-[(5-{[butyl(2-cyclohexylethyl)amino]methyl}-2'-methylbiphenyl-2-yl)carbonyl]-L-methionine

Indication

Disease Entry	ICD 11	Status	REF
Non-small-cell lung cancer	2C25.Y	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 447312
  TTD Drug ID: DM4UN9A

Molecule-Related Drug Atlas

Drug(s) Targeting Farnesyl protein transferase (Ftase)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lonafarnib	DMGM2Z6	Hutchinson-Gilford progeria syndrome	LD2B	Approved	[4]
Zarnestra	DMF30HL	Acute myeloid leukaemia	2A60	Phase 3	[5]
L-778123	DMWSC5L	Lymphoma	2A80-2A86	Phase 1	[6]
GGTI-2418	DM8U23L	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
BMS214662	DM5M48F	Non-small-cell lung cancer	2C25.Y	Phase 1	[8]
L-745631	DM4UP7R	Solid tumour/cancer	2A00-2F9Z	Terminated	[9]
MANUMYCIN A	DM1SWOY	N. A.	N. A.	Terminated	[10]
SCH-44342	DMUL4VX	N. A.	N. A.	Terminated	[11]
RPR-113829	DMJ63GW	N. A.	N. A.	Terminated	[12]
RPR-114334	DMAIJT6	N. A.	N. A.	Terminated	[12]

Drug(s) Targeting CAAX farnesyltransferase beta (FNTB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
L-745631	DM4UP7R	Solid tumour/cancer	2A00-2F9Z	Terminated	[9]
MANUMYCIN A	DM1SWOY	N. A.	N. A.	Terminated	[10]
SCH-44342	DMUL4VX	N. A.	N. A.	Terminated	[9]
RPR-113829	DMJ63GW	N. A.	N. A.	Terminated	[12]
RPR-114334	DMAIJT6	N. A.	N. A.	Terminated	[12]
L-731735	DM1XBKC	Solid tumour/cancer	2A00-2F9Z	Terminated	[9]
FUSIDIENOL	DMI1Y92	N. A.	N. A.	Terminated	[13]
ABT-100	DMPFLS5	Solid tumour/cancer	2A00-2F9Z	Terminated	[14]
B-956	DM1IO9X	Solid tumour/cancer	2A00-2F9Z	Terminated	[15]
L-739749	DMAUG0L	Solid tumour/cancer	2A00-2F9Z	Terminated	[9]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
CAAX farnesyltransferase beta (FNTB)	TT7WZIJ	FNTB_HUMAN	Inhibitor	[2]
Farnesyl protein transferase (Ftase)	TTXQKM3	FNTA_HUMAN; FNTB_HUMAN	Inhibitor	[3]

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 800014561)
• [2] Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.
• [3] Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [5] Tipifarnib in the treatment of newly diagnosed acute myelogenous leukemia. Biologics. 2008 Sep;2(3):491-500.
• [6] Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein trans... Mol Cancer Ther. 2002 Jul;1(9):747-58.
• [7] Company report (Prescient)
• [8] Farnesyltransferase inhibitor BMS-214662 induces apoptosis in B-cell chronic lymphocytic leukemia cells. Leukemia. 2004 Oct;18(10):1599-604.
• [9] Ras farnesyltransferase: a new therapeutic target. J Med Chem. 1997 Sep 12;40(19):2971-90.
• [10] A novel metal-chelating inhibitor of protein farnesyltransferase. Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.
• [11] Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. J Med Chem. 1999 Jun 17;42(12):2125-35.
• [12] Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. J Med Chem. 1997 Jun 6;40(12):1763-7.
• [13] Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking. J Med Chem. 2002 Mar 28;45(7):1460-5.
• [14] Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. J Heart Lung Transplant. 2005 Sep;24(9):1403-9.
• [15] Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. 1995 Nov 15;55(22):5310-4.