anagrelide [Ligand Id: 7114] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL760 (Agrylin, Anagrelide, Xagrid)
  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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  • phosphodiesterase 3A in Human [GtoPdb: 1298] [UniProtKB: Q14432]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of cGMP hydrolysis by human platelet phosphodiesterase F 4.47 pIC50 34000 nM IC50 J Med Chem (1991) 34: 2906-2916 [PMID:1654430]
ChEMBL Inhibition of human platelet PDE by inhibiting cyclic Guanosine monophosphate (cGMP) hydrolysis B 4.47 pIC50 34000 nM IC50 J Med Chem (1992) 35: 2672-2687 [PMID:1321910]
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
ChEMBL Inhibition of platelet aggregation using Adenosine diphosphate (ADP) as activating agent in rabbit platelet rich plasma (PRP) F 5.98 pEC50 1050 nM EC50 J Med Chem (1992) 35: 2672-2687 [PMID:1321910]
phosphodiesterase 3A in Human [GtoPdb: 1298] [UniProtKB: Q14432]
GtoPdb - - 7.27 pIC50 54 nM IC50 J Med Chem (1992) 35: 2672-87 [PMID:1321910];
J Med Chem (1987) 30: 295-303 [PMID:3027338];
J Med Chem (1992) 35: 620-8 [PMID:1311763]

ChEMBL data shown on this page come from version 32:

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]