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ChEMBL ligand: CHEMBL932 (Attia, B01AC07, Cerebrovase 100, Cerebrovase 25, Dipyridamole, Iv persantine, Modaplate, NSC-515776, Ofcram pr, Persantin, Persantine, Persantin ret, Pyridantin, RA-8, Vasyrol) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 5.16 | pIC50 | 6956 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Equilibrative nucleoside transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808] | ||||||||
ChEMBL | Displacement of 5-(SAENTA)-X8-fluorescein from K562 cell nucleoside transporter | B | 8.06 | pKi | 8.79 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2257-2260 [PMID:15081020] |
ChEMBL | Inhibition of ENT1 in human K562 cells by flow cytometric assay | B | 8.09 | pKi | 8.18 | nM | Ki | J Med Chem (2007) 50: 3906-3920 [PMID:17636949] |
GtoPdb | - | - | 8.8 | pKi | 1.5 | nM | Ki | J Pharmacol Exp Ther (2004) 308: 1083-93 [PMID:14634039] |
ChEMBL | Inhibition of ENT1 in human K562 cells by flow cytometric assay | B | 6.84 | pIC50 | 144.8 | nM | IC50 | J Med Chem (2007) 50: 3906-3920 [PMID:17636949] |
ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells | F | 5.7 | pIC50 | 2000 | nM | IC50 | Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538] |
ABCC5/Multidrug resistance-associated protein 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells | F | 4.52 | pIC50 | 30000 | nM | IC50 | Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells | F | 4.46 | pIC50 | 34300 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
ChEMBL | TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells | F | 4.63 | pIC50 | 23700 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
ChEMBL | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells | F | 4.64 | pIC50 | 22700 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
ChEMBL | Inhibitory activity against phosphodiesterase 10 | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2005) 48: 3449-3462 [PMID:15887951] |
phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9] | ||||||||
ChEMBL | Inhibition of human phosphodiesterase 11 | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2005) 48: 3449-3462 [PMID:15887951] |
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
ChEMBL | Inhibition of cyclic GMP sensitive phosphodiesterase PDE 2 of guinea pig ventricle | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (1985) 28: 537-545 [PMID:2985781] |
ChEMBL | Inhibition of cGMP-stimulated phosphodiesterase 2 of porcine coronary arteries | B | 5.44 | pIC50 | 3600 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
ChEMBL | Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets, range 2.54-4.14 | B | 5.49 | pIC50 | 3240 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
Phosphodiesterase 3A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3061] [UniProtKB: Q9XSW7] | ||||||||
ChEMBL | Inhibition of cGMP-inhibited phosphodiesterase from porcine coronary arteries | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
ChEMBL | Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets, range 31.8-60.7 | B | 4.36 | pIC50 | 44000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
Phosphodiesterase 4A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3333] [UniProtKB: O77823] | ||||||||
ChEMBL | Inhibition of cAMP specific phosphodiesterase from porcine coronary arteries | B | 5.19 | pIC50 | 6400 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
ChEMBL | Inhibition of phosphodiesterase 4 (PDE4) from porcine liver, range 0.058-7.78 | B | 5.28 | pIC50 | 5270 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
ChEMBL | DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) | B | 5.55 | pIC50 | 2831 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of phosphodiesterase 5 (PDE5) from porcine platelets, range 0.244-1.35 | B | 6.24 | pIC50 | 574 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
ChEMBL | Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta. | B | 6.28 | pIC50 | 520 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum GHA strain infected in human erythrocytes after 72 hrs by spectrophotometry | F | 4.19 | pIC50 | 64000 | nM | IC50 | J Med Chem (2011) 54: 3222-3240 [PMID:21504142] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | 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 | 5.4 | pIC50 | 3981.07 | 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 | 5.5 | pIC50 | 3162.28 | 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 | 5.5 | pIC50 | 3162.28 | 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 | 5.6 | pIC50 | 2511.89 | 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 | 5.7 | pIC50 | 1995.26 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 5.89 | pIC50 | 1300 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
Protein prune homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079850] [UniProtKB: Q86TP1] | ||||||||
ChEMBL | Inhibition of human prune assessed as reduction of cAMP-phosphodiesterase activity | B | 6.11 | pIC50 | 780 | nM | IC50 | Eur J Med Chem (2012) 57: 41-50 [PMID:23059542] |
Plasma membrane monoamine transporter in Human [GtoPdb: 1120] [UniProtKB: Q7RTT9] | ||||||||
GtoPdb | - | - | 5.9 | pKi | - | - | - | Biochem Pharmacol (2013) 86: 1531-40 [PMID:24021350] |
phosphodiesterase 7B in Human [GtoPdb: 1306] [UniProtKB: Q9NP56] | ||||||||
GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 |
Biochem Biophys Res Commun (2000) 272: 186-92 [PMID:10872825]; Biochem Biophys Res Commun (2000) 271: 575-83 [PMID:10814504] |
phosphodiesterase 8A in Human [GtoPdb: 1307] [UniProtKB: O60658] | ||||||||
GtoPdb | - | - | 5.1 | pIC50 | 7940 | nM | IC50 | Biochem Biophys Res Commun (1998) 246: 570-7 [PMID:9618252] |
phosphodiesterase 8B in Human [GtoPdb: 1308] [UniProtKB: O95263] | ||||||||
GtoPdb | - | - | 4.3 | pIC50 | 50100 | nM | IC50 | Biochem Biophys Res Commun (1998) 250: 751-6 [PMID:9784418] |
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]