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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 |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells assessed as reversal of BCRP-mediated mitoxantrone resistance and measured after 90 mins by FACSflow cytometry analysis | B | 5.19 | pIC50 | 6400 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
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] |
ChEMBL | Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay (PubChem AID: 1745861) | F | 8.09 | pIC50 | 8.1 | nM | IC50 | Sci Rep (2019) 9: 13802-null [PMID:31551431] |
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] |
phosphodiesterase 8A/Phosphodiesterase 8A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658] | ||||||||
GtoPdb | - | - | 5.1 | pIC50 | 7940 | nM | IC50 | Biochem Biophys Res Commun (1998) 246: 570-7 [PMID:9618252] |
ChEMBL | Inhibition of human recombinant PDE8A expressed in baculovirus infected Sf9 insect cells | B | 5.4 | pIC50 | 4000 | nM | IC50 | Eur J Med Chem (2021) 212: 113123-113123 [PMID:33412421] |
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 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 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]