4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide : A benzocycloheptapyridine that is benzo[5,6]cyclohepta[1,2-b]pyridine which is substituted at positions 3 and 10 by bromines, at position 8 by chlorine, and at position 11 by an N-acetylpiperidin-4-yl group in which one of the hydrogens of the acetyl moiety has been replaced by a 1-carbamoylpiperidin-4-yl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
lonafarnib: inhibitor of farnesyl protein transferase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
lonafarnib : A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase inhibitor. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 9852353 |
| CHEBI ID | 90678 |
| SCHEMBL ID | 94653 |
| MeSH ID | M0297075 |
| PubMed CID | 148195 |
| CHEMBL ID | 298734 |
| CHEBI ID | 47097 |
| SCHEMBL ID | 19032 |
| MeSH ID | M0297075 |
| Synonym |
|---|
| 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide |
| 4-[2-(4-{6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-yl}piperidin-1-yl)-2-oxoethyl]piperidine-1-carboxamide |
| bdbm14433 |
| 4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)-1-piperidinecarboxamide |
| 193275-86-4 |
| FT-0670837 |
| SCHEMBL94653 |
| CHEBI:90678 |
| HMS3656N10 |
| NCGC00389702-01 |
| Q27162641 |
| (+)-4-[2-[4-(8-chloro-3,10-dibromo-6,11-dihydro-5h-benzo[5,6]-cyclohepta[1,2-b]-pyridin-11-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide |
| SB16694 |
| lonafarnib (racemate) |
| DTXSID90870198 |
| HY-15136 |
| lonafarnib (sch66336) |
| nsc-719467 |
| (+)-4[2-[4-(8-chloro-3,11-dihydro-5h-benzo[5,6] cyclohepta[1,2-b]-pyridin-11(r)-yl-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide |
| nsc719467 |
| sch-066336 |
| lonafarnib |
| sarasar |
| D04768 |
| lonafarnib (usan/inn) |
| 193275-84-2 |
| 1O5M |
| sch-66336 |
| sch66336 |
| 1-piperidinecarboxamide, 4-(2-(4-((11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)- |
| (+)-4-(2-(4-(11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-piperidin-1-yl))-2-oxoethyl)-piperidine-1-carboxamide |
| lonafarnib [usan] |
| 1-piperidinecarboxamide, 4-(2-(4-((11r-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)- |
| 4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro-5h-benzo-(5,6)-cyclohepta(1,2-b)-pyridin-11(r)-yl)-1-piperidinyl)-2-oxo-ethyl)-1-piperidinecarboxamide |
| zokinvy |
| sch 66336 |
| (+)-4-[2-[4-(8-chloro-3,10-dibromo-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11(r)-yl)-1-piperidin-yl]-2-oxo-ethyl]-1-piperidinecarboxamide |
| bdbm14459 |
| 4-(2-{4-[(2r)-6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-yl]piperidin-1-yl}-2-oxoethyl)piperidine-1-carboxamide |
| chembl298734 , |
| AKOS005145760 |
| lonafarnib [usan:inn] |
| iow153004f , |
| unii-iow153004f |
| 4-[2-[4-[(11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide |
| NCGC00346707-01 |
| CS-0792 |
| S2797 |
| lonafarnib [inn] |
| lonafarnib [who-dd] |
| lonafarnib [mi] |
| lonafarnib [orange book] |
| gtpl8024 |
| 4-[2-[4-[(11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[1,2]cyclohepta[2,4-b]pyridin-11-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide |
| MLS006010423 |
| MLS006011106 |
| smr004701448 |
| SCHEMBL19032 |
| (r)-4-(2-(4-(3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl)-2-oxoethyl)piperidine-1-carboxamide |
| AC-32661 |
| DTXSID90172927 , |
| CHEBI:47097 , |
| 4-(2-{4-[(11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]piperidin-1-yl}-2-oxoethyl)piperidine-1-carboxamide |
| lonafarnibum |
| J-514232 |
| 4-[2-[4-[(11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidi necarboxamide |
| lonafarnib, >=98% (hplc) |
| SW220034-1 |
| BCP07027 |
| Q3258910 |
| 4-[2-[4-[(2r)-6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide |
| 4-[2-[4-(6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide |
| EX-A1630 |
| DB06448 |
| CCG-270312 |
| C73675 |
| 1-piperidinecarboxamide, 4-[2-[4-[(11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]- |
| AS-56182 |
| EN300-18167093 |
| 4-(2-{4-[(2r)-6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.0,3,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperidin-1-yl}-2-oxoethyl)piperidine-1-carboxamide |
| 4-(2-(4-((11r)-3,10-dibromo-8-chloro-6,11-dihydro-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)piperidin-1-yl)-2-oxoethyl)piperidine-1-carboxamide |
| dtxcid5095418 |
Lonafarnib (Zokinvy™) is an orally active farnesyltransferase inhibitor developed by Eiger BioPharmaceuticals under license from Merck & Co. The drug is undergoing clinical studies for the treatment of solid tumors and hematological malignancies.
Lonafarnib has been associated with diarrhea and other gastrointestinal toxicity, anorexia, and nausea. It has also demonstrated therapeutic synergy with coadministered taxanes, vincristine, cisplatin, cyclophosphamide and Gleevec.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Lonafarnib can inhibit the proliferation of imatinib-resistant cells and increases imatinib-induced apoptosis in vitro in cells from imatinib-resistant patients." | ( Phase 1 study of lonafarnib (SCH 66336) and imatinib mesylate in patients with chronic myeloid leukemia who have failed prior single-agent therapy with imatinib. Cortes, J; Daley, GQ; Ferrajoli, A; Jabbour, E; Kantarjian, H; Koller, C; O'Brien, S; Statkevich, P; Verstovsek, S; Zhu, Y, 2007) | 1.4 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with lonafarnib would therefore be predicted to be synergistic with these coadministered cancer therapeutics that are substrates of P-gp." | ( The farnesyl protein transferase inhibitor lonafarnib (SCH66336) is an inhibitor of multidrug resistance proteins 1 and 2. Johnson, WW; Wang, EJ, 2003) | 0.92 |
Lonafarnib (SCH66336) was conducted in children with recurrent or progressive CNS tumors. Intrasubject variability in the pharmacokinetic parameters was less pronounced after multiple dosing than that after single dosing.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The activity of FTi SCH66336, alone or in combination with paclitaxel, gemcitabine, and radiotherapy, was examined in 3 cell lines, A-549, LX-1 and CaLu-6, by colorimetric MTT assay." | ( In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines. Ardizzoni, A; De Cupis, A; Favoni, RE; Loprevite, M; Mazzanti, P; Scolaro, T; Semino, C, 2004) | 0.32 |
| " Promising preliminary antitumor activity warrants further evaluation of lonafarnib in combination with paclitaxel and trastuzumab in Her2-positive breast cancer." | ( Phase I study of lonafarnib (SCH66336) in combination with trastuzumab plus paclitaxel in Her2/neu overexpressing breast cancer: EORTC study 16023. Awada, A; Beijnen, JH; Diéras, V; Govaerts, AS; Huitema, AD; Kerklaan, BM; Le Tourneau, C; Marreaud, S; Mergui-Roelvink, M; Milojkovic Kerklaan, B; Piccart-Gebhart, MJ; Rosing, H; Schellens, JH, 2013) | 0.96 |
Lonafarnib is an orally bioavailable nonpetidomimetic farnesyl transferase inhibitor with significant activity against BCR-ABL-positive cell lines and primary human chronic myeloid leukemia (CML) cells.
Intermittent dosing of lonafarnib (5 days on then 5 days off) produced similar regressions in hormone-refractory 22Rv1 tumors. Coadministration could thus reduce chemotherapy dosage and hence produce lower exposure to normal cells and less undesired toxicity.
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| EC 2.5.1.58 (protein farnesyltransferase) inhibitor | An EC 2.5.1.* (non-methyl-alkyl or aryl transferase) inhibitor that interferes with the action of protein farnesyltransferase (EC 2.5.1.58), one of the three enzymes in the prenyltransferase group. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| benzocycloheptapyridine | |
| N-acylpiperidine | |
| heteroarylpiperidine | |
| organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
| organobromine compound | A compound containing at least one carbon-bromine bond. |
| ureas | |
| 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide | A benzocycloheptapyridine that is benzo[5,6]cyclohepta[1,2-b]pyridine which is substituted at positions 3 and 10 by bromines, at position 8 by chlorine, and at position 11 by an N-acetylpiperidin-4-yl group in which one of the hydrogens of the acetyl moiety has been replaced by a 1-carbamoylpiperidin-4-yl group. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.5355 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.9330 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 11.9877 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| PPM1D protein | Homo sapiens (human) | Potency | 32.9993 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 13.6389 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| polyprotein | Zika virus | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| Interferon beta | Homo sapiens (human) | Potency | 32.9993 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Mus musculus (house mouse) | EC50 (µMol) | 0.1000 | 0.0016 | 0.0338 | 0.1000 | AID246037 |
| Protein farnesyltransferase subunit beta | Mus musculus (house mouse) | EC50 (µMol) | 0.1000 | 0.0016 | 0.0338 | 0.1000 | AID246037 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1797224 | FTase Activity Assay from Article 10.1016/j.bmcl.2005.02.062: \\Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.\\ | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
| AID1797222 | FTase Activity Assay from Article 10.1016/j.bmcl.2005.03.049: \\Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.\\ | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID493017 | Wombat Data for BeliefDocking | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID54283 | inhibition of tumor colony formation in soft agar | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID54282 | Effect on Ras processing in Cos-1 monkey kidney cells expressing either H-Ras-Val 12-CVLS or H-Ras-Val12. | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID1876328 | Antiviral activity against SARS-CoV-2 inoculated in african green monkey Vero E6 cells expressing ACE2 assessed as reduction of cytopathic effect measured after 72 hrs by CellTitre-Glo based plate reader method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| AID1893921 | Bioavailability in mouse | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID13878 | Maximum concentration (Cmax) using 20%aqueous hydroxypropyl-beta-cyclodextrin (HPbetaCD) as vehicle. compound was administered orally to nude mice at a dose of 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID80387 | Compound was measured for inhibition of HCT116 tumor cell line in colon under soft agar assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID241304 | Inhibition of [3H]-FPP incorporation into H-ras CVLS by farnesyltransferase | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Farnesyl protein transferase inhibitors targeting the catalytic zinc for enhanced binding. |
| AID14027 | Bioavailability in mouse (nude) using 20% aqueous hydroxypropyl-beta-cyclodextrin (HPbetaCD) as vehicle 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID10524 | Area under curve was determined using 20%aqueous hydroxypropyl-beta-cyclodextrin (HPbetaCD) as vehicle. Compound was administered orally to nude mice at a dose of 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID240979 | Inhibition of bovine farnesyltransferase | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
| AID240536 | Inhibition of soft agar colony formation in H-Ras transformed cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID46671 | Inhibiting the farnesylation of H-ras proteins in COS-7 monkey cells transiently expressing H-ras[Val12]-CVLS in the whole cell assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID240596 | Inhibition of H-Ras transformed NIH3T3 cell proliferation | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID164302 | Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18 | Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitor |
| AID1121277 | Inhibition of human recombinant FTase using [3H]farnesyldiphosphate | 2013 | MedChemComm, Mar, Volume: 4, Issue:3 | Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections. |
| AID240944 | Inhibition of Bovine farnesyltransferase (FTase) | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors. |
| AID10520 | Area under curve was determined using 0.4% Methyl cellulose (MC) as vehicle. Compound was administered orally to nude mice at a dose of 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID103225 | Compound was measured for inhibition of MCF-7 tumor cell line in breast under soft agar assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID73272 | In vitro inhibition of human Farnesyltransferase | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase. |
| AID241103 | Inhibition of Bovine geranylgeranyltransferase (GGT) | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors. |
| AID680070 | TP_TRANSPORTER: inhibition of DNR efflux (DNR: ? uM) in MDR1-expressing NIH3T3 cells | 2001 | Cancer research, Oct-15, Volume: 61, Issue:20 | The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein. |
| AID503917 | Selectivity for protein farnesyltransferase over GGTase1 | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Therapeutic intervention based on protein prenylation and associated modifications. |
| AID19090 | Half life was administered by using 20%aqueous hydroxypropyl-beta-cyclodextrin (HPbetaCD) as vehicle to nude mice at a dose of 25mpk, | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID237855 | Oral bioavailability in rat | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID1893920 | Cmax in cynomolgus monkey | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID93992 | Compound was measured for inhibition of K-ras NIH tumor cell line under soft agar assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID526661 | Inhibition of FTase in human COS7 cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID72677 | In vitro inhibitory activity against farnesyltransferase (FTase) | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase. |
| AID246842 | Effective dose against Plasmodium falciparum | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID236382 | Area under the curve in rats by administering perorally | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID1562368 | Inhibition of FTase in human PC3 cells assessed as reduction in HDJ2 farnesylation at 1 uM measured after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13 | A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia. |
| AID468368 | Inhibition of rat farnesyl transferase after 30 mins | 2009 | Journal of natural products, Oct, Volume: 72, Issue:10 | Meroterpenes from Dichrostachys cinerea inhibit protein farnesyl transferase activity. |
| AID242512 | Inhibition of biotinylated lamin B peptide farnesylation by Plasmodium falciparum farnesyltransferase | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID14765 | Pharmacokinetic parameter area under the curve (0-48 h) for the compound was evaluated in nude cynomolgus monkeys after oral administration | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID241204 | Inhibition of bovine geranylgeranyl transferase | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
| AID10522 | Area under curve was determined using 20%aqueous hydroxypropyl-beta-cyclodextrin (HPbetaCD) as vehicle. Compound was administered intravenously to nude mice at a dose of 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID468369 | Cytotoxicity against human WM266.4 cells after 72 hrs by ATP lite assay | 2009 | Journal of natural products, Oct, Volume: 72, Issue:10 | Meroterpenes from Dichrostachys cinerea inhibit protein farnesyl transferase activity. |
| AID123002 | Percent efficacy is tested in nude mice carrying DLD-1 tumor cell lines (a human carcinoma cell line) containing mutated K-ras, by oral administration of drug at 10 mg/kg | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID144123 | Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase. |
| AID108083 | Compound was measured for inhibition of Mia Paca tumor cell line in pancreatic under soft agar assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID13875 | Maximum concentration (Cmax) using 0.4% Methyl cellulose (MC) as vehicle. compound was administered orally to nude mice at a dose of 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID73122 | Inhibition of Farnesyl protein transferase | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. |
| AID246037 | Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors. |
| AID1562370 | Inhibition of GGTase in human PC3 cells assessed as reduction in Rap1A geranylgeranylation at 1 uM measured after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13 | A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia. |
| AID16230 | Bioavailability was measured in cynomolgus monkeys. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID240597 | Inhibition of K-Ras transformed NIH3T3 cell proliferation | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID1371358 | Inhibition of rat brain FTase assessed as decrease in transfer of [3H]farnesyl from [3H]farnesyl PPi to H-Ras-CVLS after 30 mins by liquid scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
| AID123003 | Percent efficacy is tested in nude mice carrying DLD-1 tumor cell lines (a human carcinoma cell line) containing mutated K-ras, by oral administration of drug at 50 mg/kg | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID144110 | Compound ability to inhibit anchorage-independent growth of NIH-K tumor cell lines in soft agar. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID240768 | Inhibition of [3H]FPP incorporation into H-ras CVLS by Farnesyltransferase | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID1893919 | AUC in cynomolgus monkey | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID13877 | Maximum concentration (Cmax) using 20%aqueous hydroxypropyl-beta-cyclodextrin (HPbetaCD) as vehicle. compound was administered intravenously to nude mice at a dose of 25 mg/kg | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID14456 | Pharmacokinetic parameter Cmax for the compound was evaluated in nude cynomolgus monkeys after oral administration. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID144108 | Compound ability to inhibit anchorage-independent growth of NIH-H tumor cell lines in soft agar. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID251753 | Percent inhibition of H-ras processing in transformed NIH3T3 cells at 100 nM | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
| AID16231 | Bioavailability was measured in nude mice. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID143365 | Compound was measured for inhibition of NCI-HI146 tumor cell line in lung under soft agar assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID25693 | Half life period was measured in nude mice after intravenous administration | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID71309 | Inhibition of Farnesyltransferase | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors. |
| AID14764 | Pharmacokinetic parameter area under the curve (0-24 hr) for the compound was evaluated in nude mice after oral administration. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID25692 | Half life period was measured in cynomolgus monkey after intravenous administration | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID1121276 | Inhibition of human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranyl | 2013 | MedChemComm, Mar, Volume: 4, Issue:3 | Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections. |
| AID1371359 | Inhibition of rat brain GGTase1 assessed as decrease in transfer of [3H]H]geranylgeranyl from [3H]geranylgeranyl PPi to H-Ras-CVLL after 30 mins by liquid scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
| AID14457 | Pharmacokinetic parameter Cmax for the compound was evaluated in nude mice after oral administration. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID79248 | Compound was measured for inhibition of H-ras NIH tumor cell line under soft agar assay. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID73121 | Compound ability to inhibit the transfer of [3H]- farnesyl from Farnesyltransferase to H-Ras-CVLS, a process that is mediated by FPT | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID73282 | Inhibitory activity against Hras Farnesyltransferase (FPT). | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities. |
| AID73400 | Inhibitory concentration against farnesyltransferase was determined | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy? |
| AID240508 | Inhibition of COS cell proliferation | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability. |
| AID1893922 | Bioavailability in cynomolgus monkey | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346227 | Human HRAS (RAS subfamily) | 1998 | Cancer research, Nov-01, Volume: 58, Issue:21 | Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. |
| AID1346177 | Human KRAS (RAS subfamily) | 1998 | Cancer research, Nov-01, Volume: 58, Issue:21 | Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. |
| AID1346151 | Human NRAS (RAS subfamily) | 1998 | Cancer research, Nov-01, Volume: 58, Issue:21 | Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1797226 | In Vitro Enzyme Assay of FPT from Article 10.1021/jm980462b: \\(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl prote | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. |
| AID1797011 | PfPFT and Rat PFT IC50 Determination from Article 10.1021/jm0491039: \\Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.\\ | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 10 (4.52) | 18.2507 |
| 2000's | 118 (53.39) | 29.6817 |
| 2010's | 62 (28.05) | 24.3611 |
| 2020's | 31 (14.03) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (52.68) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 34 (15.18%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Reviews | 52 (23.21%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 2 (0.89%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 1 (0.45%) | 0.25% |
| Other | 6 (100.00%) | 84.16% |
| Other | 135 (60.27%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Once Daily (QD) Dosing of Lonafarnib (LNF) Co-administered With Ritonavir (RTV) for Treatment of Chronic Hepatitis D Virus Infection [NCT05229991] | Phase 3 | 30 participants (Anticipated) | Interventional | 2021-05-15 | Active, not recruiting | ||
| Phase I/II Trial of Everolimus in Combination With Lonafarnib in Progeria [NCT02579044] | Phase 1/Phase 2 | 80 participants (Anticipated) | Interventional | 2015-12-31 | Enrolling by invitation | ||
| A Pivotal Randomized Study of Lonafarnib Versus Placebo in the Treatment of Subjects With Myelodysplastic Syndrome (MDS) or Chronic Myelomonocytic Leukemia (CMML) Who Are Platelet Transfusion Dependent With or Without Anemia [NCT00109538] | Phase 3 | 47 participants (Actual) | Interventional | 2005-05-31 | Terminated | ||
| A Treatment IND (Investigational New Drug) Protocol for EAP (Expanded Access Program) for the Use of Lonafarnib in Patients With Hutchinson-Gilford Progeria Syndrome (HGPS) or Progeroid Laminopathy [NCT03895528] | 0 participants | Expanded Access | Approved for marketing | ||||
| Treatment of Chronic Delta Hepatitis With Lonafarnib, Ritonavir and Lambda Interferon [NCT03600714] | Phase 2 | 26 participants (Actual) | Interventional | 2018-08-01 | Completed | ||
| Phase I/Ib Study of Sarasar and Temodar in Patients With Recurrent or Temodar-Refractory Glioblastoma Multiforme [NCT00102648] | Phase 1 | 35 participants (Anticipated) | Interventional | 2004-12-21 | Active, not recruiting | ||
| An Open Label Dose Adjusted Phase II Trial of the Oral Farnesyltransferase Inhibitor (FTI) Lonafarnib (SCH66336) for Patients With Hutchinson-Gilford Progeria Syndrome (HGPS) and Progeroid Laminopathies [NCT00425607] | Phase 2 | 29 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
| Phase II Study on SCH 66336 (Farnesyl Protein Transferase Inhibitor) and Gemcitabine as Second Line Treatment in Advanced Metastatic Urothelial Cancer - EORTC Study 16997 [NCT00006351] | Phase 2 | 34 participants (Actual) | Interventional | 2000-06-30 | Completed | ||
| An Open-label, Dose-ranging, Proof-of-Concept Study to Evaluate the Safety and Efficacy of Lonafarnib With Ritonavir-Boosting +/- Peginterferon Alfa-2a in Patients Chronically Infected With Delta Hepatitis (HDV) (LOWR-2) [NCT02430194] | Phase 2 | 55 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
| A Phase I Trial of the Addition of the Farnesyl Transferase Inhibitor, SCH 66336, to Temodar for Patients With Grade 3 and 4 Malignant Gliomas [NCT00612651] | Phase 1 | 37 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
| An Open-Label, Two-Part Study to Determine the Safety, Tolerability, and Activity of Lonafarnib and Docetaxel [NCT00539968] | Phase 1/Phase 2 | 5 participants (Actual) | Interventional | 2007-06-30 | Terminated | ||
| Phase II Study of SCH66336, A Farnesyltransferase Inhibitor in Chronic Myelogenous Leukemia (CML) [NCT00038597] | Phase 2 | 13 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
| Defining the Interaction of Docetaxel and Lonafarnib in Patients With Advanced Malignancies [NCT00288444] | Phase 1 | 38 participants (Actual) | Interventional | 2006-01-31 | Terminated | ||
| An Open-label, Dose-ranging, Proof-of-Concept Study to Evaluate the Safety and Efficacy of Lonafarnib With and Without Ritonavir Boosting in Patients Chronically Infected With Delta Hepatitis (HDV) (LOWR-1) [NCT02430181] | Phase 2 | 21 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
| A Phase IB Clinical Study Of The Farnesyltransferase Inhibitor SCH 66336 And Gemcitabine In Patients With Resectable Primary Liver Neoplasms [NCT00020774] | Phase 2 | 0 participants (Actual) | Interventional | 1998-10-31 | Withdrawn | ||
| An Open-label, Multicenter, Randomized Phase II Study to Compare the Effects of Paclitaxel/Carboplatin and Lonafarnib to Those of Paclitaxel/Carboplatin for First-line Treatment of Patients With Epithelial Ovarian Cancer FIGO Stages IIB-IV [NCT00281515] | Phase 2 | 105 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
| Phase I Study Of SCH66336 (Lonafarnib), A Farnesyl Protein Transferase Inhibitor In Combination With Temozolomide In Gliomas [NCT00083096] | Phase 1 | 30 participants (Anticipated) | Interventional | 2004-03-31 | Active, not recruiting | ||
| A Phase IB Randomized Translational Study of Fenretinide (4-HPR) in Combination With SCH66336, a Farnesyl Transferase Inhibitor, in Patients With Advanced or Recurrent Head and Neck Cancer [NCT00102635] | Phase 1 | 1 participants (Actual) | Interventional | 2005-01-20 | Terminated(stopped due to Slow accrual.) | ||
| A Phase IB Study of Oral Administration of SCH 66336 Preoperatively in Patients With Head and Neck Squamous Cell Cancer Scheduled for Definitive Therapy [NCT00038584] | Phase 1 | 37 participants (Actual) | Interventional | 1999-06-30 | Completed | ||
| Phase I Trial Of Escalating Oral Doses Of SCH 66336 In Pediatric Patients With Refractory Or Recurrent Brain Tumors [NCT00015899] | Phase 1 | 53 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
| Phase II Evaluation Temozolomide and Farnesyl Transferase Inhibitor (SCH66336) for the Treatment of Recurrent and Progressive Glioblastoma Multiforme [NCT00038493] | Phase 2 | 23 participants (Actual) | Interventional | 2001-09-21 | Completed | ||
| A Phase 2b, Open-Label, Randomized Study of the Safety, Tolerability, and Pharmacodynamic Activity of Lonafarnib With or Without Ritonavir in Patients Chronically Infected With Hepatitis Delta Virus (LOWR-5) [NCT02968641] | Phase 2 | 0 participants (Actual) | Interventional | Withdrawn(stopped due to This study was initially planned to enroll patients in Mongolia. However, due to challenges in setting it up in Mongolia, this study was later determined not to be initiated.) | |||
| Phase I Study of Lonafarnib (SCH66336) in Combination With Herceptin Plus Paclitaxel in HER 2 NEU Overexpressing Breast Cancer [NCT00068757] | Phase 1 | 23 participants (Actual) | Interventional | 2003-08-31 | Completed | ||
| A Phase 3 Randomized Study of Lonafarnib in Combination With Paclitaxel and Carboplatin vs. Placebo in Combination With Paclitaxel and Carboplatin in Patients With Non-Small Cell Lung Cancer [NCT00050336] | Phase 3 | 702 participants (Actual) | Interventional | 2002-12-31 | Terminated | ||
| Phase I Study of Lonafarnib (SCH66336) and Gleevec (Imatinib Mesylate) in Chronic Myelogenous Leukemia (CML) [NCT00047502] | Phase 1 | 23 participants (Actual) | Interventional | 2002-11-01 | Completed | ||
| A Phase II Study of Lonafarnib in Patients With Metastatic Breast Cancer [NCT00773474] | Phase 2 | 29 participants (Actual) | Interventional | 2008-10-31 | Terminated(stopped due to funding terminated) | ||
| A Phase I Study of Continuous Oral Administration of SCH 66336 and 5-Fluorouracil/Leucovorin (5FU/LV) in Patients With Advanced Cancer [NCT00003956] | Phase 1 | 25 participants (Anticipated) | Interventional | 1999-04-30 | Completed | ||
| A Phase IB Study of Oral Administration of SCH 66336 Preoperatively in Patients With Colorectal Carcinoma Metastatic to the Liver Scheduled for Exploratory Laparotomy and/or Resection [NCT00005030] | Phase 1 | 0 participants (Actual) | Interventional | 1999-09-29 | Withdrawn(stopped due to No enrollment.) | ||
| A Phase 3, Matrix Design, Partially Double-Blind, Randomized Study of the Efficacy and Safety of 50 mg Lonafarnib/100 mg Ritonavir BID With and Without 180 mcg PEG IFN-alfa-2a for 48 Weeks Compared With PEG IFN-alfa-2a Monotherapy and Placebo Treatment in [NCT03719313] | Phase 3 | 407 participants (Actual) | Interventional | 2018-12-01 | Completed | ||
| An Open Label Phase II Trial of Zoledronic Acid, Pravastatin, and Lonafarnib for Patients With Hutchinson-Gilford Progeria Syndrome(HGPS) and Progeroid Laminopathies [NCT00916747] | Phase 2 | 85 participants (Actual) | Interventional | 2009-08-31 | Active, not recruiting | ||
| A Phase 2, Open-Label Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Activity of a Titrating-Dose Lonafarnib/Ritonavir in Patients Chronically Infected With Hepatitis Delta Virus [NCT02527707] | Phase 2 | 15 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| A Phase II Pilot Study of Zoledronic Acid, Pravastatin, and Lonafarnib (SCH66336) for Patients With Hutchinson-Gilford Progeria Syndrome (HGPS) and Progeroid Laminopathies [NCT00879034] | Phase 2 | 5 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| A Randomized Double-Blind Phase-2 Study of Anastrozole Plus Lonafarnib (SCH 66336) or Anastrozole Plus Placebo for the Treatment of Subjects With Advanced Breast Cancer [NCT00081510] | Phase 2 | 110 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
| Treatment of Chronic Delta Hepatitis With Lonafarnib [NCT01495585] | Phase 2 | 14 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
| Treatment of Chronic Delta Hepatitis With Lonafarnib and Ritonavir [NCT02511431] | Phase 2 | 22 participants (Actual) | Interventional | 2015-07-29 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||