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
Angiotensin-converting enzyme 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3736] [GtoPdb: 1614] [UniProtKB: Q9BYF1]
ChEMBL Inhibition of human recombinant ACE2 at 50 uM using (7Mca-Y-V-A- D -A-P- K(Knp) as a flurogenic substrate measured after 10 mins by fluorescence based analysis B 6.14 pIC50 720 nM IC50 J Med Chem (2020) 63: 12256-12274 [PMID:32539378]
Cyclic GMP-AMP synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105728] [GtoPdb: 3165] [UniProtKB: Q8N884]
ChEMBL Inhibition of cGAS in human THP-1 cells B 4.64 pIC50 23000 nM IC50 Eur J Med Chem (2022) 238: 114480-114480 [PMID:35635952]
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 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]