cilostazol [Ligand Id: 7148] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL799 (Cilostazol, NSC-758936, OPC-13013, OPC-21, Pletal)
  • phosphodiesterase 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
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  • phosphodiesterase 3B/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3B in Human [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
GtoPdb - - 6.7 pIC50 200 nM IC50 Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042]
ChEMBL Inhibition of PDE3A (unknown origin) using FAM-cAMP as substrate incubated for 45 mins by TR-FRET analysis B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2024) 271: 116386-116386 [PMID:38614063]
ChEMBL Inhibition of human PDE3A expressed in Sf9 cells using cAMP as substrate after 3 hrs by IMAP TR-FRET assay B 8.41 pIC50 3.89 nM IC50 Bioorg Med Chem (2020) 28: 115540-115540 [PMID:32503691]
phosphodiesterase 3B/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
GtoPdb - - 6.42 pIC50 380 nM IC50 Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042]
ChEMBL Inhibition of human recombinant PDE3B using FAM-cyclic-3',5'-AMP as substrate incubated for 1 hrs by fluorescence polarization based assay B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2024) 271: 116386-116386 [PMID:38614063]
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5 pIC50 10000 nM IC50 DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 36:

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]