salmeterol [Ligand Id: 559] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1263 (Beglan, Cryogenine, GR 33343 X, GR-33343X, GR-33343-X, Neovent, NSC-272693, Salmaterol, Salmeterol, Serevent, SN408D, Soltel, Vertine)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assay B 5.6 pKi 2511.89 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma counting B 5.64 pKi 2300 nM Ki Bioorg. Med. Chem. (2010) 18: 728-736 [PMID:20036561]
ChEMBL Displacement of [3H]CGP12177 from human beta-1 adrenoceptor B 6.1 pKi 801 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 5302-5307 [PMID:20655218]
ChEMBL Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay B 6.11 pKi 784 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
ChEMBL Binding affinity to adrenergic beta1 receptor B 6.3 pIC50 501.19 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Binding affinity to beta1 adrenoceptor B 6.3 pIC50 501.19 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 689-695 [PMID:22079756]
ChEMBL Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay B 5.3 pEC50 5011.87 nM EC50 J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
ChEMBL Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay F 5.91 pEC50 1230.27 nM EC50 Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952]
ChEMBL Agonist activity at adrenergic beta1 receptor F 6.1 pEC50 794.33 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation F 6.1 pEC50 794.33 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation F 6.1 pEC50 794.33 nM EC50 Bioorg. Med. Chem. (2011) 19: 6026-6032 [PMID:21925889]
ChEMBL Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay F 6.1 pEC50 794.33 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay B 6.1 pEC50 794.33 nM EC50 J. Med. Chem. (2014) 57: 159-170 [PMID:24359185]
ChEMBL Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins F 6.1 pEC50 794.33 nM EC50 J. Med. Chem. (2010) 53: 4522-4530 [PMID:20462258]
ChEMBL Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay F 6.6 pEC50 251.19 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
ChEMBL Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay F 6.6 pEC50 251.19 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay F 6.6 pEC50 251.19 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 1213-1218 [PMID:22178551]
ChEMBL Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay B 6.7 pEC50 199.53 nM EC50 J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
ChEMBL Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay B 6.26 pKi 550 nM Ki J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction F 8.3 pEC50 5.01 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting B 5.96 pKd 1100 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting B 9.52 pKd 0.3 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting B 6.74 pKi 184 nM Ki Bioorg. Med. Chem. (2010) 18: 728-736 [PMID:20036561]
ChEMBL Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay B 8.49 pKi 3.2 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
ChEMBL Displacement of [3H]CGP12177 from human beta2 adrenoceptor B 8.49 pKi 3.2 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 5302-5307 [PMID:20655218]
ChEMBL Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
ChEMBL Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs B 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1354-1358 [PMID:21310610]
ChEMBL Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting B 8.82 pKi 1.5 nM Ki Bioorg. Med. Chem. (2010) 18: 728-736 [PMID:20036561]
ChEMBL Binding affinity for human beta-2 adrenergic receptor B 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4705-4710 [PMID:15324892]
ChEMBL Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay B 9.41 pKi 0.39 nM Ki J. Med. Chem. (2010) 53: 3675-3684 [PMID:20402514]
ChEMBL Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay B 9.6 pKi 0.25 nM Ki J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
ChEMBL Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells B 9.74 pKi 0.18 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting B 8.3 pIC50 5.01 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1213-1218 [PMID:22178551]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins F 9.1 pEC50 0.79 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr F 9.1 pEC50 0.79 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4027-4031 [PMID:21652207]
ChEMBL Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay B 9.1 pEC50 0.79 nM EC50 J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry F 9.1 pEC50 0.79 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 689-695 [PMID:22079756]
ChEMBL Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
ChEMBL Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 1213-1218 [PMID:22178551]
ChEMBL Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay F 9.48 pEC50 0.33 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1354-1358 [PMID:21310610]
ChEMBL Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay F 9.49 pEC50 0.32 nM EC50 J. Med. Chem. (2010) 53: 3675-3684 [PMID:20402514]
ChEMBL Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay F 9.5 pEC50 0.32 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
ChEMBL Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay F 9.5 pEC50 0.32 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 1213-1218 [PMID:22178551]
ChEMBL Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay F 9.5 pEC50 0.32 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay F 9.6 pEC50 0.25 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation F 9.6 pEC50 0.25 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay F 9.6 pEC50 0.25 nM EC50 J. Med. Chem. (2014) 57: 159-170 [PMID:24359185]
ChEMBL Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation F 9.6 pEC50 0.25 nM EC50 Bioorg. Med. Chem. (2011) 19: 6026-6032 [PMID:21925889]
ChEMBL Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins F 9.6 pEC50 0.25 nM EC50 J. Med. Chem. (2010) 53: 4522-4530 [PMID:20462258]
ChEMBL Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay B 9.9 pEC50 0.13 nM EC50 J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
GtoPdb - - 9.92 pEC50 0.12 nM EC50 Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]
ChEMBL Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay B 10.1 pEC50 0.08 nM EC50 J Med Chem (2019) 62: 5111-5131 [PMID:31042379]
ChEMBL Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay F 10.11 pEC50 0.08 nM EC50 Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952]
ChEMBL Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP F 10.15 pEC50 0.07 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4012-4015 [PMID:17498952]
ChEMBL Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels F 10.15 pEC50 0.07 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 6188-6191 [PMID:17897826]
ChEMBL Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method F 10.15 pEC50 0.07 nM EC50 J. Med. Chem. (2010) 53: 6640-6652 [PMID:20804199]
ChEMBL Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay F 10.35 pEC50 0.04 nM EC50 Bioorg Med Chem (2020) 28: 115178-115178 [PMID:31753798]
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
ChEMBL Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins F 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2010) 53: 3675-3684 [PMID:20402514]
ChEMBL Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction B 8.46 pIC50 3.5 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
ChEMBL Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction B 7.5 pEC50 31.62 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction F 8.3 pEC50 5.01 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response F 8.3 pEC50 5.01 nM EC50 Bioorg. Med. Chem. (2011) 19: 6026-6032 [PMID:21925889]
ChEMBL Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction B 8.57 pEC50 2.7 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 5121-5126 [PMID:26471092]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay F 5.9 pEC50 1258.93 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins F 5.9 pEC50 1258.93 nM EC50 J. Med. Chem. (2010) 53: 4522-4530 [PMID:20462258]
ChEMBL Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation F 5.9 pEC50 1258.93 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation F 5.9 pEC50 1258.93 nM EC50 Bioorg. Med. Chem. (2011) 19: 6026-6032 [PMID:21925889]
ChEMBL Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay B 5.9 pEC50 1258.93 nM EC50 J. Med. Chem. (2014) 57: 159-170 [PMID:24359185]
ChEMBL Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells B 4.49 pKi 32000 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [125I]7-HO-PIPAT from human D3R expressed in HEK cells B 5.98 pKi 1049 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]

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]