compound 89S [PMID: 19115845] [Ligand Id: 8114] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL524266
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
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  • cell division cycle 7/Cell division cycle 7-related protein kinase in Human [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • High affinity immunoglobulin gamma Fc receptor I in Human [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
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  • inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 11/MAP kinase p38 beta in Human [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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  • STE20 like kinase/Serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
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  • NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
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  • serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
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  • p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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  • cyclin dependent kinase 1 in Human [GtoPdb: 1961] [UniProtKB: P06493]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of ALK B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
ChEMBL Inhibition of PKAalpha B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311]
GtoPdb - - 9.3 pKi 0.5 nM Ki J Med Chem (2009) 52: 293-307 [PMID:19115845]
ChEMBL Inhibition of human Cdc7 assessed as inhibition of rate of phosphorylation of Mcm2 protein B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
GtoPdb - - 8.7 pIC50 2 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
GtoPdb CDK2/cyclin A complex - 6.86 pIC50 138 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
ChEMBL Inhibition of Cdk2A B 6.86 pIC50 138 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibition of CDK4 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of CDK5/p25 B 5.79 pIC50 1620 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
GtoPdb CDK9/cyclin T complex - 7.55 pIC50 28 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
ChEMBL Inhibition of CDK9 B 7.55 pIC50 28 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3-beta B 6.84 pIC50 146 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
GtoPdb - - 6.84 pIC50 146 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of MET B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
High affinity immunoglobulin gamma Fc receptor I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
ChEMBL Inhibition of IGFR1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
ChEMBL Inhibition of IKKi B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of IR B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of MK2 B 6.29 pIC50 510 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 B 6.07 pIC50 846 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
mitogen-activated protein kinase 11/MAP kinase p38 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
ChEMBL Inhibition of P38beta B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of TRKA B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of PKCbeta B 5.94 pIC50 1149 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
ChEMBL Inhibition of PDK1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
STE20 like kinase/Serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
ChEMBL Inhibition of STLK2 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of AKT1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of AUR2 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
ChEMBL Inhibition of AUR1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of CHK1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL Inhibition of MST4 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
ChEMBL Inhibition of NEK6 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
ChEMBL Inhibition of NIM1 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
GtoPdb - - 5.4 pIC50 >4000 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Inhibition of PAK4 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 B 6.24 pIC50 574 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
ChEMBL Inhibition of TAO3 B 6.9 pIC50 126 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
GtoPdb - - 6.9 pIC50 126 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of KIT B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of VEGFR3 B 5.4 pIC50 >4000 nM IC50 J. Med. Chem. (2009) 52: 293-307 [PMID:19115845]
cyclin dependent kinase 1 in Human [GtoPdb: 1961] [UniProtKB: P06493]
GtoPdb CDK1/cyclin B complex - 7.52 pIC50 30 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]