hydroxychloroquine [Ligand Id: 7198] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1535 (Hydroxychloroquine, Polirreumin)
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.63 pKi 2346 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.32 pIC50 4772 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine B 5.19 pKi 6456.54 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Activity of compound against Alpha 2B (ADRA2B) adrenergic receptor by displacement of [3H]-rauwolscine B 4.14 pKi 72443.6 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine B 4.8 pKi 15848.93 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
Genome polyprotein in Zika virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523954] [UniProtKB: A0A024AXB9]
ChEMBL Inhibition of Zika virus NS2B-NS3 protease B 4.03 pKi 92300 nM Ki Bioorg Med Chem Lett (2020) 30: 126965-126965 [PMID:31980339]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M1 (CHRM1) by displacement of 3H-QNB B 4.81 pKi 15488.17 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M2 (CHRM2) by displacement of 3H-QNB B 5.29 pKi 5128.61 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.98 pKi 1049 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.53 pIC50 2951 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB B 5.32 pKi 4786.3 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB B 5.26 pKi 5495.41 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M5 (CHRM5) by displacement of 3H-QNB B 4.7 pKi 19952.62 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake preincubated for 24 hrs followed by [G-3H]hypoxanthine addition and measured after 18 to 24 hrs by scintillation spectrometry F 5.65 pIC50 2217 nM IC50 Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum T996 infected in human erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake preincubated for 24 hrs followed by [G-3H]hypoxanthine addition and measured after 18 to 24 hrs by scintillation spectrometry F 7.67 pIC50 21.5 nM IC50 Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL Displacement of [3H]-DTG from the Sigma2 receptor B 6 pKi 1000 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Displacement of [3H]-pentazocin from the Sigma1 receptor B 6.9 pKi 125.89 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
TLR7/Toll-like receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5936] [GtoPdb: 1757] [UniProtKB: Q9NYK1]
ChEMBL Antagonist activity at human TLR7 expressed in HEK-Blue cells assessed as inhibition of CL264-induced NFkappaB activation by measuring reduction in SEAP level after overnight incubation using qunati-blue reagent by SEAP reporter gene-based spectrophotometric method B 5.07 pIC50 8600 nM IC50 J Med Chem (2020) 63: 4776-4789 [PMID:32302115]
GtoPdb Inhibition of hTLR7 R848-induced luciferase reporter gene activation. - 5.56 pIC50 2780 nM IC50 Mol Pharmacol (2014) 85: 429-40 [PMID:24342772]
ChEMBL Antagonist activity at human TLR7 expressed in HEK-Blue cells assessed as reduction in CL264-induced NF-kappaB levels after 24 hrs by spectrophotometric analysis B 6.1 pIC50 800 nM IC50 Eur J Med Chem (2018) 159: 187-205 [PMID:30292896]
ChEMBL Antagonist activity at TLR7 (unknown origin) B 6.1 pIC50 800 nM IC50 Eur J Med Chem (2021) 210: 112978-112978 [PMID:33189437]
TLR9/Toll-like receptor 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5804] [GtoPdb: 1759] [UniProtKB: Q9NR96]
ChEMBL Antagonist activity at human TLR9 expressed in HEK-Blue cells assessed as reduction in CpGB-induced NF-kappaB levels after 24 hrs by spectrophotometric analysis B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2018) 159: 187-205 [PMID:30292896]
GtoPdb Inhibition of hTLR9 CpG2006-induced luciferase reporter gene activation. - 7.1 pIC50 80 nM IC50 Mol Pharmacol (2014) 85: 429-40 [PMID:24342772]

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]