General Information of Drug (ID: DMWSC5L)

Drug Name
L-778123 Drug Info
Synonyms
183499-57-2; L-778123; UNII-31ZXM8ZKQ3; 4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]METHYL}-1H-IMIDAZOL-1-YL)METHYL]BENZONITRILE; 31ZXM8ZKQ3; CHEMBL279433; 4-((5-((4-(3-chlorophenyl)-3-oxopiperazin-1-yl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile; L-778123 free base; 4-[[5-[[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl]imidazol-1-yl]methyl]benzonitrile; 4-[(5-{[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl}imidazol-1-yl)methyl]benzonitrile; SCHEMBL1683541; AC1L50Q0; CTK7C7787; 1s63; 1s64; BDBM50097071; ZINC53070632
Indication
Disease Entry ICD 11 Status REF
Lymphoma 2A80-2A86 Phase 1 [1]
Cross-matching ID
PubChem CID
216454
CAS Number
CAS 183499-57-2
TTD Drug ID
DMWSC5L

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lonafarnib DMGM2Z6 Hutchinson-Gilford progeria syndrome LD2B Approved [3]
Zarnestra DMF30HL Acute myeloid leukaemia 2A60 Phase 3 [4]
GGTI-2418 DM8U23L Solid tumour/cancer 2A00-2F9Z Phase 1 [5]
BMS214662 DM5M48F Non-small-cell lung cancer 2C25.Y Phase 1 [6]
L-745631 DM4UP7R Solid tumour/cancer 2A00-2F9Z Terminated [7]
ABT-839 DM4UN9A Non-small-cell lung cancer 2C25.Y Terminated [8]
MANUMYCIN A DM1SWOY N. A. N. A. Terminated [9]
SCH-44342 DMUL4VX N. A. N. A. Terminated [10]
RPR-113829 DMJ63GW N. A. N. A. Terminated [11]
RPR-114334 DMAIJT6 N. A. N. A. Terminated [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
L-745631 DM4UP7R Solid tumour/cancer 2A00-2F9Z Terminated [7]
GGTI-298 DM1CG0J N. A. N. A. Terminated [12]
PD-83176 DMSIMKZ Discovery agent N.A. Investigative [13]
A-313326 DML4P6O Discovery agent N.A. Investigative [14]
J-109,390 DM9SFGB Discovery agent N.A. Investigative [15]
L-269,289 DMV6018 Discovery agent N.A. Investigative [15]
⏷ Show the Full List of 6 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Farnesyl protein transferase (Ftase) TTXQKM3 FNTA_HUMAN; FNTB_HUMAN Modulator [2]
Geranylgeranyl transferase I (GGTase-I) TTX20QP PGTB1_HUMAN Modulator [2]

References

1 ClinicalTrials.gov (NCT00003430) L-778,123 in Treating Patients With Recurrent or Refractory Solid Tumors. U.S. National Institutes of Health.
2 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.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
4 Tipifarnib in the treatment of newly diagnosed acute myelogenous leukemia. Biologics. 2008 Sep;2(3):491-500.
5 Company report (Prescient)
6 Farnesyltransferase inhibitor BMS-214662 induces apoptosis in B-cell chronic lymphocytic leukemia cells. Leukemia. 2004 Oct;18(10):1599-604.
7 Ras farnesyltransferase: a new therapeutic target. J Med Chem. 1997 Sep 12;40(19):2971-90.
8 Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62.
9 A novel metal-chelating inhibitor of protein farnesyltransferase. Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.
10 Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. J Med Chem. 1999 Jun 17;42(12):2125-35.
11 Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. J Med Chem. 1997 Jun 6;40(12):1763-7.
12 The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. J Biol Chem. 1997 Oct 24;272(43):27224-9.
13 Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. J Med Chem. 1997 Jan 17;40(2):192-200.
14 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.
15 Geranylgeranyltransferase I of Candida albicans: null mutants or enzyme inhibitors produce unexpected phenotypes. J Bacteriol. 2000 Feb;182(3):704-13.