zaprinast [Ligand Id: 2919] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL28079 (M&B 22948, NSC-757885, Zaprinast) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| ChEMBL | Competitive binding affinity to Nluc-fused human GPR35 expressed in CHO-K1 cells assessed as inhibition constant using furimazine as substrate incubated for 30 mins followed by substrate addition by in presence of 10-(4-(2-(4-(4-((2,8-dicarboxy-6-hydroxy-10-methylpyrido[3,2-g]quinolin-4-yl)oxy)butyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-5,5-difluoro-2,7,9-trimethyl-5H-imidazo[1,2-c]pyrrolo[2,1-f][1,3,2]diazaborinin-6-ium-5-uide | B | 6.21 | pKi | 612 | nM | Ki | ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394] |
| ChEMBL | Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (2013) 56: 7084-7099 [PMID:23888932] |
| ChEMBL | Antagonist activity at GPR35 in human HT-29 cells assessed as inhibition of zaprinast-induced DMR by dynamic mass redistribution assay | F | 4.98 | pIC50 | 10500 | nM | IC50 | J Med Chem (2011) 54: 7385-7396 [PMID:21950657] |
| ChEMBL | Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution assay | F | 5.91 | pIC50 | 1220 | nM | IC50 | J Med Chem (2011) 54: 7385-7396 [PMID:21950657] |
| ChEMBL | Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins | B | 5.91 | pIC50 | 1220 | nM | IC50 | ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447] |
| ChEMBL | Agonist activity at human GPR35 receptor expressed in CHO-K1 cells assessed as desensitization of zaprinast-induced DMR response preincubated for 1 hr followed by zaprinast stimulation by DMR desensitization assay | F | 7.32 | pIC50 | 48.15 | nM | IC50 | J Med Chem (2021) 64: 2634-2647 [PMID:33630609] |
| ChEMBL | Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay | F | 5.21 | pEC50 | 6200 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4148-4152 [PMID:22572579] |
| ChEMBL | Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay | F | 5.21 | pEC50 | 6100 | nM | EC50 | ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447] |
| ChEMBL | Agonist activity at human GPR35 expressed in U2OS cells coexpressing Gal4-VP16/beta-arrestin fusion protein after 5 hrs by tango beta-arrestin translocation reporter gene assay | F | 5.28 | pEC50 | 5300 | nM | EC50 | ACS Med Chem Lett (2012) 3: 550-554 [PMID:24900508] |
| ChEMBL | Agonist activity at human GPR35 expressed in CHO-K1 cells after 90 mins by beta-arrestin 2 recruitment assay | B | 5.38 | pEC50 | 4200 | nM | EC50 | J Med Chem (2017) 60: 362-372 [PMID:27976894] |
| ChEMBL | Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcriptional activation after 5 hrs by tango beta-arrestin translocation reporter assay | F | 5.38 | pEC50 | 4200 | nM | EC50 | J Med Chem (2011) 54: 7385-7396 [PMID:21950657] |
| ChEMBL | Agonist activity at TEV protease cleavage site linked GAL4-VP16-fused GPR35 in human Tango GPR35-bla U2OS cells assessed as induction of TEV protease-tagged beta-arrestin recruitment incubated for 5 hrs by beta-lactamase reporter gene assay | B | 5.45 | pEC50 | 3520 | nM | EC50 | J Med Chem (2017) 60: 362-372 [PMID:27976894] |
| ChEMBL | Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay | B | 5.49 | pEC50 | 3250 | nM | EC50 | Medchemcomm (2012) 3: 1270-1274 |
| ChEMBL | Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay | B | 5.65 | pEC50 | 2240 | nM | EC50 | J Med Chem (2013) 56: 5182-5197 [PMID:23713606] |
| ChEMBL | Agonist activity at human GPR35 assessed as induction of beta-arrestin recruitment | F | 5.7 | pEC50 | 2000 | nM | EC50 | ACS Med Chem Lett (2018) 9: 422-427 [PMID:29795753] |
| ChEMBL | Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay | B | 5.71 | pEC50 | 1960 | nM | EC50 | J Med Chem (2013) 56: 5182-5197 [PMID:23713606] |
| GtoPdb | - | - | 6.1 | pEC50 | - | - | - | FEBS Lett (2006) 580: 5003-8 [PMID:16934253] |
| ChEMBL | Agonist activity at human GPR35 receptor expressed in HT-29 cells assessed as dynamic mass redistribution response by DMR assay | F | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (2021) 64: 2634-2647 [PMID:33630609] |
| ChEMBL | Agonist activity at GPR35 in human HT-29 cells by DMR assay | B | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (2017) 60: 362-372 [PMID:27976894] |
| ChEMBL | Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay | F | 6.8 | pEC50 | 160 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4148-4152 [PMID:22572579] |
| ChEMBL | Agonist activity at human GPR35 expressed in CHO-K1 cells by DMR assay | B | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2017) 60: 362-372 [PMID:27976894] |
| ChEMBL | Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assay | F | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2011) 54: 7385-7396 [PMID:21950657] |
| ChEMBL | Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay | F | 6.8 | pEC50 | 160 | nM | EC50 | ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447] |
| ChEMBL | Agonist activity at GPR35 in human HT-29 cells measured after 10 mins by dynamic mass redistribution assay | F | 6.85 | pEC50 | 140 | nM | EC50 | ACS Med Chem Lett (2012) 3: 550-554 [PMID:24900508] |
| ChEMBL | Agonist activity at human GPR35 by Ca+2 release assay | B | 6.89 | pEC50 | 130 | nM | EC50 | J Med Chem (2013) 56: 7084-7099 [PMID:23888932] |
| ChEMBL | Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis | B | 6.96 | pEC50 | 110 | nM | EC50 | Medchemcomm (2012) 3: 1270-1274 |
| ChEMBL | Agonist activity at human GPR35 receptor expressed in CHO-K1 cells assessed as dynamic mass redistribution response by DMR assay | F | 7.2 | pEC50 | 62.83 | nM | EC50 | J Med Chem (2021) 64: 2634-2647 [PMID:33630609] |
| ChEMBL | Agonist activity at GPR-35 in human HT-29 cells by DMR assay | B | 9.15 | pEC50 | 0.71 | nM | EC50 | ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394] |
| GPR35/G-protein coupled receptor 35 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2390813] [GtoPdb: 102] [UniProtKB: Q9ES90] | ||||||||
| ChEMBL | Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay | B | 6.01 | pEC50 | 980 | nM | EC50 | J Med Chem (2013) 56: 5182-5197 [PMID:23713606] |
| GPR35 in Rat [GtoPdb: 102] [UniProtKB: Q33BM1] | ||||||||
| GtoPdb | - | - | 7.8 | pEC50 | - | - | - | FEBS Lett (2006) 580: 5003-8 [PMID:16934253] |
| GPR35 in Human [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| GtoPdb | - | - | 6.1 | pEC50 | - | - | - | FEBS Lett (2006) 580: 5003-8 [PMID:16934253] |
| GPR35/G protein-coupled receptor GPR35 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2390812] [GtoPdb: 102] [UniProtKB: Q33BM1] | ||||||||
| ChEMBL | Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay | B | 7.21 | pEC50 | 61.1 | nM | EC50 | J Med Chem (2013) 56: 5182-5197 [PMID:23713606] |
| GtoPdb | - | - | 7.8 | pEC50 | - | - | - | FEBS Lett (2006) 580: 5003-8 [PMID:16934253] |
| phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
| ChEMBL | Inhibitory concentration value against phosphodiesterase 10 | B | 4.66 | pIC50 | 22000 | nM | IC50 | 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 | 4.92 | pKi | 12000 | nM | Ki | J Med Chem (2005) 48: 3449-3462 [PMID:15887951] |
| phosphodiesterase 1C/Phosphodiesterase 1C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4619] [GtoPdb: 1296] [UniProtKB: Q14123] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 1C at 100 uM | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (1994) 37: 476-485 [PMID:8120866] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets, range 68.1-119 | B | 4.04 | pIC50 | 90200 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| ChEMBL | Inhibition of cGMP-stimulated phosphodiesterase 2 of porcine coronary arteries | B | 4.33 | pIC50 | 46800 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
| ChEMBL | Inhibition of human recombinant PDE2 (phosphodiesterase 2) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 4525-4532 [PMID:14521414] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062] | ||||||||
| ChEMBL | Inhibition of rat brain Phosphodiesterase 2 | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (1995) 38: 3547-3557 [PMID:7658441] |
| ChEMBL | Inhibition of rat brain particulate cGMP phosphodiesterase | B | 4.2 | pIC50 | 63100 | nM | IC50 | J Med Chem (1982) 25: 1192-1198 [PMID:6292419] |
| Phosphodiesterase 3A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3061] [UniProtKB: Q9XSW7] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| 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] |
| Phosphodiesterase 3B in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5129] [UniProtKB: E1BN64] | ||||||||
| ChEMBL | Inhibition of bovine aorta PDE3 (phosphodiesterase 3) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 4525-4532 [PMID:14521414] |
| phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4AL (PDE4AL) in baculovirus expression system | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| Phosphodiesterase 4A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3333] [UniProtKB: O77823] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 4 (PDE4) from porcine liver | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| ChEMBL | Inhibition of cAMP specific phosphodiesterase from porcine aorta | B | 4.1 | pIC50 | 79600 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
| phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4BL (PDE4BL) in baculovirus expression system | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4DE (PDE4DE) in baculovirus expression system | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4D3 (PDE4D3) in baculovirus expression system | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4D5 (PDE4D5) in baculovirus expression system | B | 5.06 | pKi | 8760 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| ChEMBL | Inhibition of human phosphodiesterase 5 | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2005) 48: 3449-3462 [PMID:15887951] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 5.5 | pIC50 | 3162.28 | nM | IC50 | J Med Chem (2018) 61: 6421-6467 [PMID:29620890] |
| ChEMBL | Inhibitory activity against phosphodiesterase 5 from human platelets | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 3547-3557 [PMID:7658441] |
| ChEMBL | Inhibition of Phosphodiesterase 5 from human corpus cavernosum | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1819-1824 |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2018) 61: 6421-6467 [PMID:29620890] |
| ChEMBL | Inhibition of human corpus cavernosum PDE5 | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2020) 63: 15153-15186 [PMID:33314936] |
| ChEMBL | Inhibition of PDE5 | B | 5.7 | pIC50 | 1995.26 | nM | IC50 | Bioorg Med Chem (2008) 16: 7599-7606 [PMID:18656371] |
| ChEMBL | DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) | B | 5.87 | pIC50 | 1349 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of phosphodiesterase 5 (PDE5) from porcine platelets, range 0.733-1.68 | B | 5.95 | pIC50 | 1110 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| ChEMBL | In vitro inhibition of PDE-V isolated from porcine pulmonary artery. | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1993) 36: 1387-1392 [PMID:8388468] |
| ChEMBL | Concentration required to inhibit 50% activity of phosphodiesterase VA isoenzyme at 100 uM | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (1994) 37: 476-485 [PMID:8120866] |
| ChEMBL | Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta. | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
| ChEMBL | In vitro inhibition of phosphodiesterase (PDE V). | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 89-94 |
| ChEMBL | Inhibition of Phosphodiesterase 5 from human | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1996) 39: 1635-1644 [PMID:8648603] |
| GtoPdb | - | - | 6.8 | pIC50 | 158 | nM | IC50 | Mol Pharmacol (1999) 56: 124-30 [PMID:10385692] |
| Phosphodiesterase 5A in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304402] [UniProtKB: O77746] | ||||||||
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 6.12 | pIC50 | 760 | nM | IC50 | J Med Chem (2013) 56: 5182-5197 [PMID:23713606] |
| Phosphodiesterase 5A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3478] [UniProtKB: Q28156] | ||||||||
| ChEMBL | Inhibition of bovine platelet PDE5 | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3983-3987 [PMID:22607677] |
| ChEMBL | Evaluated for inhibitory activity against Phosphodiesterase 5 (PDE5) purified from bovine lung | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (1997) 40: 2196-2210 [PMID:9216839] |
| ChEMBL | Inhibition of bovine aortic smooth muscle PDE5 using cGMP as substrate incubated for 30 mins in presence of EGTA and [3H]cGMP by liquid scintillation counting method | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2019) 177: 269-290 [PMID:31158744] |
| ChEMBL | Inhibitory activity against bovine PDE5 (phosphodiesterase-5). | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2003) 46: 4525-4532 [PMID:14521414] |
| phosphodiesterase 5A/Phosphodiesterase 5A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4567] [GtoPdb: 1304] [UniProtKB: O54735] | ||||||||
| ChEMBL | Compound was tested for inhibition of stimulation of rat aortic smooth muscle cells (RSMC) | F | 5.05 | pEC50 | 9000 | nM | EC50 | J Med Chem (1996) 39: 1635-1644 [PMID:8648603] |
| phosphodiesterase 9A/Phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083] | ||||||||
| ChEMBL | Inhibition of human phosphodiesterase 9 | B | 4.46 | pKi | 35000 | nM | Ki | J Med Chem (2005) 48: 3449-3462 [PMID:15887951] |
| GtoPdb | - | - | 4.5 | pIC50 | 31600 | nM | IC50 | J Biol Chem (1998) 273: 15559-64 [PMID:9624146] |
| Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653] | ||||||||
| ChEMBL | HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells | F | 5.11 | pIC50 | 7790 | nM | IC50 | Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | HARVARD: Inhibition of blood stage Plasmodium falciparum 3D7 infection | F | 4.3 | pIC50 | >50000 | nM | IC50 | Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124] |
| ChEMBL | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum GHA strain infected in human erythrocytes after 72 hrs by spectrophotometry | F | 4.46 | pIC50 | 35000 | nM | IC50 | J Med Chem (2011) 54: 3222-3240 [PMID:21504142] |
| ChEMBL | HARVARD: Inhibition of blood stage Plasmodium falciparum Dd2 infection | F | 4.71 | pIC50 | 19300 | nM | IC50 | Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 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] |
| mitochondrial pyruvate carrier 2 in Human [GtoPdb: 3023] [UniProtKB: O95563] | ||||||||
| GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Mol Metab (2022) 60: 101469 [PMID:35278701] |
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]
