cycloheximide [Ligand Id: 5433] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL123292 (Cicloheximida, Cicloheximide, Cycloheximide, GNF-Pf-5118, NSC-171, NSC-185, TCMDC-125838, U-4527)
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  • FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942]
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  • FKBP prolyl isomerase 4/FK506 binding protein 4 in Human [ChEMBL: CHEMBL4050] [GtoPdb: 3176] [UniProtKB: Q02790]
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  • Glucose transporter in Leishmania mexicana [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
  • Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
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  • Hexose transporter 1 in Plasmodium falciparum [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Eukaryotic initiation factor 4A-I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2052028] [UniProtKB: P60842]
ChEMBL Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat AGAGAG in 5'- UTR containing luciferase reporter gene assay B 6.65 pIC50 226 nM IC50 J Med Chem (2020) 63: 5879-5955 [PMID:32470302]
ChEMBL Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CAACAA in 5'- UTR containing luciferase reporter gene assay B 6.85 pIC50 142 nM IC50 J Med Chem (2020) 63: 5879-5955 [PMID:32470302]
ChEMBL Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat GGCGGC in 5'- UTR containing luciferase reporter gene assay B 7 pIC50 101 nM IC50 J Med Chem (2020) 63: 5879-5955 [PMID:32470302]
ChEMBL Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CCGCCG in 5'- UTR containing luciferase reporter gene assay B 7.06 pIC50 87 nM IC50 J Med Chem (2020) 63: 5879-5955 [PMID:32470302]
FK506 binding protein 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2342] [UniProtKB: Q9NWM8]
ChEMBL Inhibition constant(Ki) for inhibition of PPIase activity of Photobacterium sp. FK506 binding protein 22 (Conc=41 nM) of FKBPs family B 4.12 pKi 76200 nM Ki J Med Chem (1999) 42: 3615-3622 [PMID:10479292]
FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942]
ChEMBL Inhibition constant(Ki) for inhibition of PPIase activity of human FK506 binding protein 12 (Conc=14 nM) of FKBPs family B 5.47 pKi 3400 nM Ki J Med Chem (1999) 42: 3615-3622 [PMID:10479292]
ChEMBL Binding affinity to FKBP12 (unknown origin) B 5.47 pKi 3400 nM Ki J Med Chem (2016) 59: 9622-9644 [PMID:27409354]
ChEMBL Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay B 5.44 pIC50 3600 nM IC50 J Med Chem (1999) 42: 3615-3622 [PMID:10479292]
GtoPdb - - 5.47 pIC50 3400 nM IC50 J Med Chem (1999) 42: 3615-22 [PMID:10479292]
FKBP prolyl isomerase 4/FK506 binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4050] [GtoPdb: 3176] [UniProtKB: Q02790]
ChEMBL Inhibition constant(Ki) for inhibition of PPIase activity of rabbit FK506 binding protein 52 (Conc=52 nM) of FKBPs family B 4.62 pKi 24200 nM Ki J Med Chem (1999) 42: 3615-3622 [PMID:10479292]
Glucose transporter in Leishmania mexicana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGT2 that are glucose transport deficient and complemented with the L. Mexicana glucose transporter 2. Activity is measured by by DNA content using SYBR green in vitro F 6.62 pIC50 242 nM IC50 St. Jude Leishmania screening dataset.
Glucose transporter 1/Glucose transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGLUT1 that are glucose transport deficient and complemented with the human glucose transporter GLUT1. Activity is measured by DNA content using SYBR green in vitro F 6.64 pIC50 228 nM IC50 St. Jude Leishmania screening dataset.
Hexose transporter 1 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmPfHT that are glucose transport deficient and complemented with the Plasmodium falciparum hexose transporter. Activity is measured by by DNA content using SYBR green in vitro F 6.51 pIC50 310 nM IC50 St. Jude Leishmania screening dataset.
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells F 7.33 pIC50 47 nM IC50 Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green based fluorescence assay F 6.49 pIC50 320 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone2 bearing P-type ATPase4 T418N and P990R mutations after 72 hrs by SYBR green based fluorescence assay F 6.51 pIC50 310 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone3 bearing P-type ATPase4 D1247Y mutations after 72 hrs by SYBR green based fluorescence assay F 6.52 pIC50 301 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone1 bearing P-type ATPase4 I398F and P990R mutations after 72 hrs by SYBR green based fluorescence assay F 6.54 pIC50 287 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum assessed as [35S]Met/Cys incorporation by SYBR green based fluorescence assay F 6.7 pIC50 200 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 48 hrs F 6.82 pIC50 150 nM IC50 Antimicrob Agents Chemother (2007) 51: 307-316 [PMID:17060533]
ChEMBL Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 96 hrs F 7 pIC50 100 nM IC50 Antimicrob Agents Chemother (2007) 51: 307-316 [PMID:17060533]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay F 6.74 pEC50 181.7 nM EC50 Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay F 6.95 pEC50 113.5 nM EC50 Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783]
Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration F 7.11 pIC50 78.1 nM IC50 Science (2011) 334: 1372-1377 [PMID:22096101]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]