cilostamide [Ligand Id: 5167] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL34431 (Cilostamide, OPC-3689)
  • phosphodiesterase 2A/Phosphodiesterase 2A in Rat [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062]
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  • phosphodiesterase 3A/Phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
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  • phosphodiesterase 3B/Phosphodiesterase 3B in Human [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 2A/Phosphodiesterase 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062]
ChEMBL Inhibitory concentration against phosphodiesterase 2 from rat kidney B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2004) 14: 2955-2958 [PMID:15125967]
phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
GtoPdb - - 7.5 pIC50 31.6 nM IC50 Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042]
ChEMBL Inhibition of human recombinant PDE3A B 7.74 pIC50 18.1 nM IC50 Bioorg Med Chem Lett (2011) 21: 1617-1620 [PMID:21330134]
ChEMBL Inhibitory concentration required to inhibit human phosphodiesterase 3A expressed in Escherichia coli B 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (2003) 13: 3983-3987 [PMID:14592490]
phosphodiesterase 3B/Phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
ChEMBL Inhibition of human recombinant PDE3B B 7.16 pIC50 69.07 nM IC50 Bioorg Med Chem Lett (2011) 21: 1617-1620 [PMID:21330134]
GtoPdb - - 7.3 pIC50 50.1 nM IC50 Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042]
ChEMBL Inhibitory concentration required to inhibit human phosphodiesterase 3B expressed in Escherichia coli B 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (2003) 13: 3983-3987 [PMID:14592490]
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibitory concentration against phosphodiesterase 5 (PDE5) from human platelet B 5.15 pIC50 7150 nM IC50 Bioorg Med Chem Lett (2004) 14: 2955-2958 [PMID:15125967]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
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 W2 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 3D7 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 GB4 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 7G8 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 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 5.6 pIC50 2511.89 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
ChEMBL DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF) B 5.72 pKi 1917 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF) B 5.43 pIC50 3687 nM IC50 DrugMatrix in vitro pharmacology data

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]