suramin [Ligand Id: 1728] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL265502 (Farma, FARMA-939, Fourneau, Metaret, Naganol, NSC-34936, Suramin, Suramine)
  • 6-phospho-1-fructokinase in Trypanosoma brucei [ChEMBL: CHEMBL5686] [UniProtKB: O15648]
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  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • ectonucleoside triphosphate diphosphohydrolase 2/Ectonucleoside triphosphate diphosphohydrolase 2 in Rat [ChEMBL: CHEMBL3300] [GtoPdb: 2889] [UniProtKB: O35795]
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  • Ectonucleoside triphosphate diphosphohydrolase 8 in Human [ChEMBL: CHEMBL5338] [UniProtKB: Q5MY95]
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  • Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
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  • sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
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  • sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
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  • sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
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  • Nucleoside triphosphate diphosphohydrolase 3 in Rat [ChEMBL: CHEMBL1075237] [UniProtKB: Q80Z26]
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  • protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
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  • P2Y11 receptor/Purinergic receptor P2Y11 in Human [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Rat [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
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  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
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  • P2Y1 receptor in Human [GtoPdb: 323] [UniProtKB: P47900]
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  • P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
6-phospho-1-fructokinase in Trypanosoma brucei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5686] [UniProtKB: O15648]
ChEMBL Inhibition of Trypanosoma brucei PFK-mediated ADP production using ATP/fructose-6-phosphate as substrate by luciferase based luminescence assay B 5.52 pIC50 3000 nM IC50 ACS Med Chem Lett (2014) 5: 12-17 [PMID:24900769]
cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858]
ChEMBL Inhibition of human liver cathepsin B B 4.52 pIC50 >30000 nM IC50 J Med Chem (2008) 51: 545-552 [PMID:18173229]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibitory activity against DNA-DNA dependent protein kinase (DNA-PK) B 5.77 pIC50 1700 nM IC50 J Med Chem (2003) 46: 1478-1483 [PMID:12672248]
ectonucleoside triphosphate diphosphohydrolase 2/Ectonucleoside triphosphate diphosphohydrolase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3300] [GtoPdb: 2889] [UniProtKB: O35795]
ChEMBL Inhibition of rat recombinant NTPDase2 expressed in CHO cells B 4.18 pKi 65400 nM Ki Bioorg Med Chem Lett (2006) 16: 5943-5947 [PMID:16997558]
ChEMBL Inhibition of rat NTPDase 2 B 4.18 pKi 65400 nM Ki J Med Chem (2008) 51: 4518-4528 [PMID:18630897]
Ectonucleoside triphosphate diphosphohydrolase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5338] [UniProtKB: Q5MY95]
ChEMBL Inhibition of human NTPDase 8 expressed in COS7 cells B 4 pKi >100000 nM Ki J Med Chem (2008) 51: 4518-4528 [PMID:18630897]
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
ChEMBL Inhibition of purified HIV-2 reverse transcriptase B 4.82 pIC50 15000 nM IC50 J Med Chem (1992) 35: 4846-4853 [PMID:1282569]
ChEMBL Inhibition of purified HIV-1 reverse transcriptase B 5.03 pIC50 9400 nM IC50 J Med Chem (1992) 35: 4846-4853 [PMID:1282569]
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
ChEMBL Inhibition of SIRT1 (unknown origin) using AMC-Arg-His-Lys-Lys(Ac) substrate assessed as deacetylation of substrate by fluorimetric enzyme assay B 5.55 pIC50 2800 nM IC50 Bioorg Med Chem Lett (2015) 25: 2768-2772 [PMID:26025875]
ChEMBL Inhibition of human SIRT1 using Fluor-de-Lys as substrate B 5.55 pIC50 2800 nM IC50 Bioorg Med Chem Lett (2012) 22: 3256-3260 [PMID:22464458]
ChEMBL In Vitro Biological Assay: 50 uM of substrate peptide (acetylated AMC-labeled peptide from p53 residues 379-382, RHKKAc, BioMol. Cat. #KI-177), 91 nM of human SIRT1 (full length human Sirtuin 1 expressed in E. coli, BioMol. Cat. #SE-239) and 500 uM NAD+ in the assay buffer (50 mM Tris-HCl, pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2 supplemented with 1 mg/ml BSA for dilution, BioMol. Cat. #KI-143) and 1% final concentration of DMSO were incubated in the presence of gradient concentrations of test compounds (10-dose with 3-fold serial dilution) at 30 C. for 2 h. The reactions were carried out in a 96-well microplate for fluorometry in a 50 ul reaction volume. After the deacetylation reaction, Fluor-de-Lys-Developer II (BioMol. Cat. #KI-176) was added to each well to digest the deacetylated substrate, thus producing the fluorescent signal. The reaction was allowed to develop for 45 minutes at 30 C. with 5% CO2; then the fluorescent signal was measured with an excitation wavelength at 360 nm. B 5.58 pIC50 2620 nM IC50 US-8835659-B2. Polysubstituted benzofurans and medicinal applications thereof (2014)
ChEMBL Inhibition of full length recombinant human SIRT1 expressed in Escherichia coli BL21 (DE3) PLysS using Fluor-de-Lys as substrate by fluorimetric assay B 5.59 pIC50 2600 nM IC50 Bioorg Med Chem Lett (2012) 22: 6160-6165 [PMID:22929231]
ChEMBL Inhibition of human full length SIRT1 expressed in DE3 cells by fluorimetric assay B 6.22 pIC50 600 nM IC50 Bioorg Med Chem (2009) 17: 7031-7041 [PMID:19734050]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged full length SIRT1 expressed in Escherichia coli BL21(DE3) using ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay B 6.52 pIC50 300 nM IC50 Medchemcomm (2010) 1: 114-124
ChEMBL Inhibition of human GST-tagged SIRT1 expressed in Escherichia coli BL21(DE3) assessed as inhibition of ZMAL conversion to ZML after 4 hrs by fluorescence assay B 6.52 pIC50 300 nM IC50 J Med Chem (2013) 56: 3666-3679 [PMID:23570514]
ChEMBL Inhibition of recombinant SIRT1 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay B 6.52 pIC50 300 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Inhibition of human His6-tagged SIRT2 expressed in Escherichia coli BL21(DE3) assessed as inhibition of ZMAL conversion to ZML after 4 hrs by fluorescence assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2013) 56: 3666-3679 [PMID:23570514]
ChEMBL Inhibition of recombinant SIRT2 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay B 5.96 pIC50 1100 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
ChEMBL Inhibition of SIRT5 using ZK(suc)A substrate after 1 hr by homogeneous fluorescence assay B 4.33 pIC50 46600 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL Inhibition of SIRT5 B 4.57 pIC50 27000 nM IC50 J Med Chem (2012) 55: 5582-5590 [PMID:22583019]
ChEMBL Inhibition of human SIRT5 assessed as reduction in desuccinylase activity using KQTAR(SuK)STGGKA substrate B 4.6 pIC50 25000 nM IC50 Bioorg Med Chem Lett (2015) 25: 1671-1674 [PMID:25818461]
ChEMBL Inhibition of human SIRT5 using H3K9 succinyl peptide substrate B 4.6 pIC50 25000 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL Inhibition of human recombinant SIRT5 isoform 1 (34 to 302 amino acids) expressed in Escherichia coli BL21 (DE3) codon plus RIL cells assessed as reduction in deacetylase activity using acetylated chicken histone substrate and [3H]-NAD+ B 4.66 pIC50 22000 nM IC50 Bioorg Med Chem Lett (2015) 25: 1671-1674 [PMID:25818461]
ChEMBL Inhibition of human Sirt5 deacetylation activity using FKRGVL-acetylLys-EYGVKV as substrate after 60 mins by glutamate dehydrogenase-coupled assay B 4.85 pIC50 14200 nM IC50 Bioorg Med Chem Lett (2013) 23: 143-146 [PMID:23195732]
ChEMBL Inhibition of SIRT5 (unknown origin) using (DABCYL)ISGASE(SuK)DIVHSE(EDANS)G peptide substrate incubated for 1 hrs followed by 1 hr incubation with trypsin and nicotinamide by HPLC-based assay B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem Lett (2015) 25: 1671-1674 [PMID:25818461]
ChEMBL Inhibition of SIRT5 (unknown origin) using (DABCYL)ISGASE(SuK)DIVHSE(EDANS)G peptide substrate incubated for 1 hrs followed by 1 hr incubation with trypsin and nicotinamide by FRET-based assay B 5.7 pIC50 2000 nM IC50 Bioorg Med Chem Lett (2015) 25: 1671-1674 [PMID:25818461]
Nucleoside triphosphate diphosphohydrolase 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075237] [UniProtKB: Q80Z26]
ChEMBL Inhibition of rat recombinant NTPDase3 expressed in CHO cells B 4.9 pKi 12700 nM Ki Bioorg Med Chem Lett (2006) 16: 5943-5947 [PMID:16997558]
P2X1/P2X purinoceptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2530] [GtoPdb: 478] [UniProtKB: P47824]
GtoPdb - - 6 pIC50 1000 nM IC50 J Med Chem (2002) 45: 4057-93 [PMID:12213051]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 1 (P2X1) at 1 uM, expressed in Xenopus oocytes F 6 pEC50 1000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X2/P2X purinoceptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2135] [GtoPdb: 479] [UniProtKB: P49653]
ChEMBL Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte assessed as inhibition of alpha, beta-meATP-induced inward current by two-electrode voltage-clamp electrophysiology F 4.4 pIC50 39810.72 nM IC50 J Med Chem (2011) 54: 817-830 [PMID:21207957]
GtoPdb - - 4.98 pIC50 10400 nM IC50 J Med Chem (2002) 45: 4057-93 [PMID:12213051]
ChEMBL Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte assessed as inhibition of alpha, beta-meATP-induced inward current by two-electrode voltage-clamp electrophysiology F 5.4 pIC50 4000 nM IC50 J Med Chem (2011) 54: 817-830 [PMID:21207957]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) at 30 uM, expressed in Xenopus oocytes F 4.98 pEC50 10400 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373]
GtoPdb - - 4.83 pIC50 14900 nM IC50 J Med Chem (2002) 45: 4057-93 [PMID:12213051]
ChEMBL Antagonist activity against recombinant human P2X purinoceptor 3 (P2X3 ) F 4.83 pEC50 14900 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 3 (P2X2) at 10 uM, expressed in Xenopus oocytes F 5.52 pEC50 3000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X3 in Rat [GtoPdb: 480] [UniProtKB: P49654]
GtoPdb - - 5.52 pIC50 3000 nM IC50 J Med Chem (2002) 45: 4057-93 [PMID:12213051]
P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577]
ChEMBL Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 3 uM, expressed in Xenopus oocytes F 4 pEC50 >100000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X5/P2X purinoceptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2495] [GtoPdb: 482] [UniProtKB: P51578]
GtoPdb - - 5.4 pIC50 4000 nM IC50 J Med Chem (2002) 45: 4057-93 [PMID:12213051]
ChEMBL Antagonist activity against recombinant rat P2X purinoceptor 5 (P2X5) F 5.4 pEC50 4000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X6/P2X purinoceptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2122] [GtoPdb: 483] [UniProtKB: P51579]
ChEMBL Antagonist activity against recombinant rat P2X purinoceptor 6 (P2X6 ) F 4 pEC50 >100000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7) F 4.04 pEC50 92000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2Y purinoceptor 1 in Turkey (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5720] [UniProtKB: P49652]
ChEMBL Evaluated for antagonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of turkey erythrocytes F 5 pEC50 >10000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
ChEMBL Inhibition of human recombinant GST-PRMT1 expressed in BL21 cells B 4.74 pIC50 18100 nM IC50 J Med Chem (2007) 50: 1241-1253 [PMID:17323938]
ChEMBL Inhibition of His6x-tagged PRMT1-mediated protein arginine methylation expressed in Escherichia coli BL21 (DE3) using H4(1-20) and [14C]-SAM by scintillation counting B 5.27 pIC50 5330 nM IC50 J Med Chem (2010) 53: 6028-6039 [PMID:20666457]
P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
ChEMBL Inhibitory concentration against P2Y purinoceptor 11 expressed in 1321N1 astrocytoma cells; n=6 B 6.52 pKi 302 nM Ki J Med Chem (2005) 48: 7040-7048 [PMID:16250663]
ChEMBL Inhibitory concentration against P2Y purinoceptor 11 expressed in 1321N1 astrocytoma cells; n=3 B 6.95 pKi 112.2 nM Ki J Med Chem (2005) 48: 7040-7048 [PMID:16250663]
GtoPdb - - 6 pIC50 - - - Br J Pharmacol (1999) 128: 1199-206 [PMID:10578132]
ChEMBL The compound was evaluated for antagonist activity against phospholipase C coupled human P2Y purinoceptor 11 (P2Y11) F 4.8 pEC50 16000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2Y12 receptor/Purinergic receptor P2Y12 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
ChEMBL Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12) F 5.4 pEC50 4000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
GtoPdb - - 4.3 pIC50 - - - Br J Pharmacol (1997) 121: 338-44 [PMID:9154346];
Br J Pharmacol (1999) 127: 709-16 [PMID:10401562]
ChEMBL Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader F 4.3 pIC50 50000 nM IC50 J Med Chem (2008) 51: 4518-4528 [PMID:18630897]
ChEMBL Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2) F 4.32 pEC50 48000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
ChEMBL The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4) F 4 pEC50 >100000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
ChEMBL Antagonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced intracellular calcium mobilization by NOVOstar plate reader F 4.57 pIC50 27000 nM IC50 J Med Chem (2008) 51: 4518-4528 [PMID:18630897]
RmtA in Emericella nidulans (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075069] [UniProtKB: Q5VLE3]
ChEMBL Inhibition of Aspergillus nidulans recombinant GST-RmtA expressed in BL21 cells B 5.23 pIC50 5900 nM IC50 J Med Chem (2007) 50: 1241-1253 [PMID:17323938]
P2Y1 receptor in Human [GtoPdb: 323] [UniProtKB: P47900]
GtoPdb - - 5.3 pKi - - - Mol Pharmacol (2002) 62: 1249-57 [PMID:12391289]
P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8]
GtoPdb - - 5.6 pIC50 - - - Mol Pharmacol (2003) 64: 104-12 [PMID:12815166]

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]