| Assay ID | Title | Year | Journal | Article |
|---|
| AID73278 | Inhibition of human farnesyltransferase in PSN-1 cells. | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. |
| AID1719307 | Potentiation of vorinostat-induced reactivation of latent HIV-1 infected in human Jurkat 2C4 cells assessed as increase in HIV-1 transcription incubated for 24 hrs in presence of vorinostat by Steady-Glo luciferase reporter gene assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID1893898 | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID74779 | In vitro inhibition against human Geranylgeranyl transferase type I catalyzed by incorporation of [3H]- GGPP (geranylgeranyl pyrophosphate) into biotinylated peptide corresponding to the c-terminus of human Ki-Ras | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID1719296 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 2 mM DMA-PP by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID23791 | Half life value of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| AID1719297 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 1 mM DMA-PP by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID72660 | Inhibition of Farnesyl protein transferase radiolabel [1-3H] incorporation | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
| The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases. |
| 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. |
| AID681355 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
| In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
| AID74503 | Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATP | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
| The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases. |
| AID1719292 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 5 mM phosphate by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID157175 | Effective dose required for half-maximal inhibition of farnesylated protein (HDJ2) in PSN-1 cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID1719306 | Reactivation of latent HIV-1 infected in human Jurkat 2C4 cells assessed as increase in HIV-1 transcription incubated for 24 hrs by Steady-Glo luciferase reporter gene assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID73257 | Concentration required to displace 50% of a radiolabeled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cells | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| 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. |
| AID1893893 | Binding affinity to NRAS (unknown origin) assessed as inhibition constant | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID1893866 | Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID1857624 | Inhibition of Cryptococcus neoformans farnesyltransferase assessed as inhibition of farnesylation of dansyl-GCVVM peptide using fluorescent peptide dansyl-GCVVM and 1uM farnesyl diphosphate as substrate by fluorescence assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase. |
| AID157055 | Minimal concentration required to inhibit Rap 1a processing (prenylation) in PSN-1 cell | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID1719293 | Inhibition of rat recombinant FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 5 mM thiosulfate by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID73271 | In vitro inhibition against human Farnesyltransferase catalyzed by incorporation of [3H]- FPP into recombinant Ras-CVIM | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID74928 | Inhibition of Geranylgeranyl transferase type I | 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. |
| AID1719294 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 5 mM ATP by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| 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? |
| AID166242 | Inhibition of colony formation in v-H-ras-transformed RAT1 cells | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID73548 | Inhibition of human Farnesyltransferase -catalyzed incorporation of [3H]FPP into recombinant Ras-CVIM. | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID8919 | Maximal plasma concentration required for pharmacokinetic data in dogs at dose of 1 mg/kg perorally | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| AID681154 | TP_TRANSPORTER: cell accumulation in KB-3-1 and KB-V1 cells | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
| In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
| AID1857639 | Inhibition of rat farnesyltransferase assessed as inhibition of farnesylation of dansyl-GCVVM peptide using fluorescent peptide dansyl-GCVVM and 1uM farnesyl diphosphate as substrate by fluorescence assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase. |
| AID1893894 | Binding affinity to HRAS (unknown origin) assessed as inhibition constant | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID73096 | Inhibition of Farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM. | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9
| Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID181374 | Concentration at which 80% cultured cells remain viable assessed by MTT staining | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| AID1719291 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 5 mM pyrophosphate by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID90410 | Slope between log (IC50) versus log [GGPP] in GGTase-I | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID8334 | Pharmacokinetic data in dogs at dose of 1 mg/kg perorally, and the area under curve (AUC) was reported. | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| AID1719298 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID1857625 | Antifungal activity against Cryptococcus neoformans H99 assessed as decrease in cell viability by measuring metabolic activity incubated for 72 hrs by alamar blue staining based broth dilution method | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase. |
| AID1719305 | Potentiation of vorinostat-induced reactivation of latent HIV-1 infected in human Jurkat 2C4 cells assessed as increase in HIV-1 transcription incubated for 24 hrs in presence of vorinostat by Steady-Glo luciferase reporter gene assay relative to control | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID1719295 | Inhibition of recombinant rat FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 5 mM DMA-PP by scintillation proximity assay | 2021 | ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
| Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen. |
| AID1893895 | Antiproliferative activity against human cancer cell lines harboring KRAS mutation assessed as reduction in cell viability | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID1893899 | Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID74650 | Inhibition of the human Geranylgeranyl transferase type I catalyzed incorporation of [3H]GGPP into a biotinylated peptide corresponding to the C-terminus of human K-Ras; Not determined. | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9
| Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID19210 | Partition coefficient (logP) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| AID157174 | Effective concentration required to inhibit K-ras processing in PSN-1 cells | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy? |
| AID74644 | Inhibition of Geranylgeranyl transferase type I | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy? |
| AID89945 | Minimum inhibitory concentration required to inhibit Rap1a processing in PSN-1 cells. | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID73567 | Inhibition of Farnesyltransferase in cells, evaluated in a radiotracer assay for farnesyltransferase inhibition (CRAFTI), in cultured H-ras-transformed Rat cells | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. |
| AID157177 | Effective dose required for half-maximal inhibition of prenylation in PSN-1 cells (Ki-Ras) | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID157179 | Ratio of effective concentration required for protein processing of Ki-Ras to that of HDJ2 in PSN-1 cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID74798 | Inhibition of human Geranylgeranyl transferase type I incorporation of [3H]GGPP into biotinylated peptide corresponding to the C-terminus of human Ki-Ras. | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID73547 | Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells. | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID72974 | Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells. | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9
| Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID157176 | Effective dose required for half-maximal inhibition of geranylgeranylated protein (Rap1a) in PSN-1 cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. |
| AID166380 | Inhibition of RAT1 v-Ha-ras-transformed cell growth in soft agar | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| AID1893896 | Antiproliferative activity against human cancer cell lines harboring wild type RAS mutation assessed as reduction in cell viability | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID681165 | TP_TRANSPORTER: transepithelial transport (basal to apical) in mdr1a-expressing LLC-PK1 cell | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
| In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
| 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. |
| AID1893897 | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway. |
| AID73261 | Inhibition of [3H]FPP incorporation into recombinant Ras-CVIM by human farnesyl transferase | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
| Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. |
| 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. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2004 | Biochemistry, Jul-20, Volume: 43, Issue:28
| Crystallographic analysis reveals that anticancer clinical candidate L-778,123 inhibits protein farnesyltransferase and geranylgeranyltransferase-I by different binding modes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |