ChEMBL ligand: CHEMBL1496 (Creston, Rosuvastatin, Rosuvastatina, Rosuvastatine, X-plended, ZD-4522, ZD4522)
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035] hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 6D/Phosphodiesterase 6D in Human [ChEMBL: CHEMBL3860] [GtoPdb: 1315] [UniProtKB: O43924] 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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
ChEMBL	Binding affinity to HMG-CoA reductase by isothermal calorimetry	B	7.77	pKd	17	nM	Kd	J Med Chem (2008) 51: 3804-3813 [PMID:18540668]
ChEMBL	Inhibitory constant against HMG-CoA reductase with alpha asarone	B	4.15	pKi	71000	nM	Ki	Bioorg Med Chem Lett (2005) 15: 989-994 [PMID:15686898]
GtoPdb	-	-	8.64	pKi	2.3	nM	Ki	Biochemistry (2005) 44: 11741-8 [PMID:16128575]
ChEMBL	Inhibitory constant against HMG-CoA reductase	B	9.05	pKi	0.9	nM	Ki	Bioorg Med Chem Lett (2005) 15: 989-994 [PMID:15686898]
ChEMBL	Inhibitory concentration against HMG-CoA reductase	B	8.27	pIC50	5.4	nM	IC50	Bioorg Med Chem Lett (2005) 15: 989-994 [PMID:15686898]
GtoPdb	in vitro inhibition of cholesterol synthesis	-	8.27	pIC50	5.4	nM	IC50	Am J Cardiol (2001) 87: 28B-32B [PMID:11256847]
GtoPdb	-	-	8.3	pIC50	5	nM	IC50	Science (2001) 292: 1160-4 [PMID:11349148]
ChEMBL	Inhibitory concentration against 3-hydroxy-3-methylglutaryl-CoA reductase	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1027-1032 [PMID:15686906]
ChEMBL	Reductase Assay : The following procedure was followed using a HMG-CoA Reductase assay kit obtained from Sigma-Aldrich (catalogue number CS1090). The assay is based on the spectrophotometric measurement of the decrease in absorbance at 340 nm of NADPH in solution. A decrease in absorbance is caused by the oxidation of NADPH by the catalytic subunit of HMGR in the presence of the substrate HMG-CoA. Effective inhibition of the HMG-CoA leads to a reduction in oxidation of NADPH which in turn leads to a smaller reduction in the absorbance at 340 nm over time.	B	8.4	pIC50	4	nM	IC50	US-9102656-B2. Use of rosuvastatin lactols as medicaments (2015)
ChEMBL	Inhibition of HMG-CoA reductase	B	8.51	pIC50	3.1	nM	IC50	Bioorg Med Chem Lett (2007) 17: 4538-4544 [PMID:17574412]
GtoPdb	Inhibition of HMG-CoA reductase	-	8.51	pIC50	3.1	nM	IC50	Bioorg Med Chem Lett (2007) 17: 4538-44 [PMID:17574412]
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639]
ChEMBL	Reductase Assay: All assays were carried out in a reaction buffer containing 100 nM KxPO4 at pH 7.2, 1 mM EDTA, 500 mM KCl and 1 mg/ml BSA. The concentrations of NADPH and HMG-CoA were both 200 μM. The enzyme concentration used is unknown although this concentration is 10-fold lower than that of the stock solution purchased. Inhibitors were dissolved in 75% DMSO. Where inhibitors were found to be insoluble or only partly soluble in 75% DMSO, 100% DMSO was used. Reactions were activated by the addition of enzyme and agitated for 12 seconds following the addition. Absorbance readings were then taken every 20 seconds for 600 seconds. In initial tests the concentration of each inhibitor was set at 50 nM to identify which compounds were the better inhibitors, compared to the known Pravastatin inhibitor.	B	8.4	pIC50	4	nM	IC50	US-9006282-B2. Rosuvastatin and atorvastatin derivatives (2015)
ChEMBL	Inhibition of rat microsomal HMGCoA reductase	B	8.43	pIC50	3.7	nM	IC50	Bioorg Med Chem Lett (2008) 18: 1151-1156 [PMID:18155906]
ChEMBL	Inhibition of rat microsomal HMG-CoA reductase assessed as inhibition of cholesterol synthesis after 30 mins	B	8.44	pIC50	3.6	nM	IC50	Bioorg Med Chem (2007) 15: 5576-5589 [PMID:17560788]
ChEMBL	Inhibition of HMG-CoA reductase in Sprague-Dawley rat liver microsomes	B	8.51	pIC50	3.1	nM	IC50	J Med Chem (2008) 51: 31-45 [PMID:18072721]
ChEMBL	Inhibition of HMGR in rat hepatic microsomes assessed as conversion of [14C]HMG-CoA to [14C]mevalonic acid	B	8.51	pIC50	3.1	nM	IC50	J Med Chem (2008) 51: 2722-2733 [PMID:18412317]
ChEMBL	Inhibition of HMG-CoA reductase in Sprague-Dawley rat liver microsomes using [14C]HMG-CoA as substrate preincubated for 0.5 hrs before substrate addition measured after 0.75 hrs by beta scintillation counting	B	8.51	pIC50	3.1	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2725-2731 [PMID:21183342]
ChEMBL	Inhibition of HMG-CoA reductase in rat liver microsomes	B	8.68	pIC50	2.1	nM	IC50	Bioorg Med Chem Lett (2007) 17: 5567-5572 [PMID:17764936]
GtoPdb	Inhibition of cholesterol systhesis	-	9.8	pIC50	0.16	nM	IC50	Am J Cardiol (2001) 87: 28B-32B [PMID:11256847]
phosphodiesterase 6D/Phosphodiesterase 6D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3860] [GtoPdb: 1315] [UniProtKB: O43924]
ChEMBL	Binding affinity to His6-tagged PDE-delta (unknown origin) measured every 3 mins by fluorescence polarization assay	B	5.9	pKd	1250	nM	Kd	J Med Chem (2014) 57: 5435-5448 [PMID:24884780]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as Plasmodium lactate dehydrogenase release after 48 hrs by colorimetry	F	4.1	pIC50	80000	nM	IC50	Antimicrob Agents Chemother (2009) 53: 2212-2214 [PMID:19258270]
ChEMBL	Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as Plasmodium lactate dehydrogenase release after 48 hrs by colorimetry	F	4.1	pIC50	80000	nM	IC50	Antimicrob Agents Chemother (2009) 53: 2212-2214 [PMID:19258270]
ChEMBL	Antimalarial activity against chloroquine-resistant Plasmodium falciparum E8B assessed as Plasmodium lactate dehydrogenase release after 48 hrs by colorimetry	F	4.1	pIC50	80000	nM	IC50	Antimicrob Agents Chemother (2009) 53: 2212-2214 [PMID:19258270]

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]