cycloheximide | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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cycloheximide
Ligand Activity Charts

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

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ChEMBL ligand: CHEMBL123292 (Cicloheximide, Cycloheximide, GNF-Pf-5118, NSC-171, NSC-185, TCMDC-125838, U-4527)
Eukaryotic initiation factor 4A-I in Human [ChEMBL: CHEMBL2052028] [UniProtKB: P60842] There should be some charts here, you may need to enable JavaScript!
FK506 binding protein 14 in Human [ChEMBL: CHEMBL2342] [UniProtKB: Q9NWM8] There should be some charts here, you may need to enable JavaScript!
FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942] There should be some charts here, you may need to enable JavaScript!
FKBP prolyl isomerase 4/FK506 binding protein 4 in Human [ChEMBL: CHEMBL4050] [GtoPdb: 3176] [UniProtKB: Q02790] There should be some charts here, you may need to enable JavaScript!
Glucose transporter in Leishmania mexicana [ChEMBL: CHEMBL3431938] [UniProtKB: O61059] Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166] There should be some charts here, you may need to enable JavaScript!
Hexose transporter 1 in Plasmodium falciparum [ChEMBL: CHEMBL4697] [UniProtKB: O97467] There should be some charts here, you may need to enable JavaScript!
Plasmodium berghei [ChEMBL: CHEMBL612653] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Plasmodium yoelii [ChEMBL: CHEMBL612889] There should be some charts here, you may need to enable JavaScript!

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	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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]