amiodarone [Ligand Id: 2566] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL633 (Amiodarona, Amiodarone, Cordarone, L-3428, Pacerone, SKF 33134-A)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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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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  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Anthrax lethal factor in Bacillus anthracis [ChEMBL: CHEMBL4372] [UniProtKB: P15917]
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • B2 receptor/Bradykinin B2 receptor in Human [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • carnitine palmitoyltransferase 1B/Carnitine O-palmitoyltransferase 1, muscle isoform in Human [ChEMBL: CHEMBL2216739] [GtoPdb: 3250] [UniProtKB: Q92523]
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  • carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Human [ChEMBL: CHEMBL3238] [GtoPdb: 3252] [UniProtKB: P23786]
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  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • CCR4/C-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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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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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • lysine demethylase 5A/Lysine-specific demethylase 5A in Human [ChEMBL: CHEMBL2424504] [GtoPdb: 2680] [UniProtKB: P29375]
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  • lysine demethylase 7A/Lysine-specific demethylase 7 in Human [ChEMBL: CHEMBL2163177] [GtoPdb: 2686] [UniProtKB: Q6ZMT4]
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  • PHD finger protein 2/Lysine-specific demethylase PHF2 in Human [ChEMBL: CHEMBL4295672] [GtoPdb: 2697] [UniProtKB: O75151]
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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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  • sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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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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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
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  • squalene monooxygenase/Squalene monooxygenase in Human [ChEMBL: CHEMBL3592] [GtoPdb: 2433] [UniProtKB: Q14534]
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  • squalene synthase /Squalene synthetase in Human [ChEMBL: CHEMBL3338] [GtoPdb: 645] [UniProtKB: P37268]
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  • Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
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  • Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • Kv1.7 in Human [GtoPdb: 544] [UniProtKB: Q96RP8]
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  • Nav1.5 in Rat [GtoPdb: 582] [UniProtKB: P15389]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
ChEMBL Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand B 7.6 pKi 25 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5 pKi 9918 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.76 pIC50 17547 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 DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.93 pKi 117 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.51 pIC50 312 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.23 pKi 5886 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 4.89 pIC50 12893 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.55 pKi 28165 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.37 pIC50 42248 nM IC50 DrugMatrix in vitro pharmacology data
Anthrax lethal factor in Bacillus anthracis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4372] [UniProtKB: P15917]
ChEMBL Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay B 5.46 pIC50 3500 nM IC50 Antimicrob Agents Chemother (2007) 51: 2403-2411 [PMID:17485504]
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 4.6 pKi 25202 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 4.36 pIC50 43643 nM IC50 DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.5 pKi 31761 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.37 pIC50 42349 nM IC50 DrugMatrix in vitro pharmacology data
B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
ChEMBL DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin) B 5.11 pKi 7674 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin) B 4.89 pIC50 12966 nM IC50 DrugMatrix in vitro pharmacology data
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
ChEMBL Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 7.21 pKi 62 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
carnitine palmitoyltransferase 1B/Carnitine O-palmitoyltransferase 1, muscle isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2216739] [GtoPdb: 3250] [UniProtKB: Q92523]
ChEMBL Inhibition of human CPT1B B 4 pIC50 >100000 nM IC50 J Med Chem (2011) 54: 3109-3152 [PMID:21504156]
carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3238] [GtoPdb: 3252] [UniProtKB: P23786]
ChEMBL Inhibition of human CPT2 B 4 pIC50 >100000 nM IC50 J Med Chem (2011) 54: 3109-3152 [PMID:21504156]
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1) B 5.37 pKi 4285 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1) B 4.96 pIC50 11086 nM IC50 DrugMatrix in vitro pharmacology data
CCR4/C-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
ChEMBL DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) B 4.94 pKi 11405 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) B 4.66 pIC50 21773 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.55 pKi 2825 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.1 pIC50 8014 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.34 pKi 4571 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.04 pIC50 9142 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.18 pKi 6651 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 4.7 pIC50 19952 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.39 pKi 410 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.92 pIC50 1208 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 5.21 pKi 6213 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 4.75 pIC50 17720 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.7 pKi 1990 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.6 pIC50 2505 nM IC50 DrugMatrix in vitro pharmacology data
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
ChEMBL DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1) B 4.79 pKi 16177 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1) B 4.58 pIC50 26288 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 5 pIC50 10000 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 6 pIC50 1000 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of potassium current (Ikr) measured using whole-cell patch clamp experiments in HEK-293 cells stable transfected with hERG cDNA F 7.52 pIC50 30 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 4.98 pKi 10379 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 4.98 pIC50 10555 nM IC50 DrugMatrix in vitro pharmacology data
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.18 pKi 6672 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.78 pIC50 16680 nM IC50 DrugMatrix in vitro pharmacology data
lysine demethylase 5A/Lysine-specific demethylase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424504] [GtoPdb: 2680] [UniProtKB: P29375]
ChEMBL Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from recombinant His6-tagged human KDM5A (PHD3) (1542 to 1660 residues) expressed in Escherichia coli 2(DE3)pLysS Rosetta competent cells preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay B 4 pIC50 99000 nM IC50 Bioorg Med Chem (2018) 26: 2984-2991 [PMID:29764755]
lysine demethylase 7A/Lysine-specific demethylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163177] [GtoPdb: 2686] [UniProtKB: Q6ZMT4]
ChEMBL Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7A (PHD-JmjC) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay B 4.1 pIC50 80000 nM IC50 Bioorg Med Chem (2018) 26: 2984-2991 [PMID:29764755]
PHD finger protein 2/Lysine-specific demethylase PHF2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295672] [GtoPdb: 2697] [UniProtKB: O75151]
ChEMBL Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7C (PHD) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay B 4.08 pIC50 84000 nM IC50 Bioorg Med Chem (2018) 26: 2984-2991 [PMID:29764755]
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
ChEMBL DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.97 pKi 10797 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.91 pIC50 12372 nM IC50 DrugMatrix in vitro pharmacology data
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.88 pKi 13226 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.86 pIC50 13755 nM IC50 DrugMatrix in vitro pharmacology data
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 5.05 pKi 8909 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 5.02 pIC50 9497 nM IC50 DrugMatrix in vitro pharmacology data
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.11 pKi 7728 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.72 pIC50 19037 nM IC50 DrugMatrix in vitro pharmacology data
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.2 pKi 629 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.58 pIC50 2613 nM IC50 DrugMatrix in vitro pharmacology data
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.74 pKi 1806 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.29 pIC50 5080 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 DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.17 pKi 679 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.49 pIC50 3201 nM IC50 DrugMatrix in vitro pharmacology data
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.3 pKi 506 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.44 pIC50 3630 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.97 pKi 1077 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.82 pIC50 1499 nM IC50 DrugMatrix in vitro pharmacology data
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
ChEMBL Activation of recombinant human SIRT3 assessed as lysyl deacetylase activity using (Gln-Pro-Lys-Lys(Ac)) peptide substrate by fluorescent assay B 5.49 pEC50 3250 nM EC50 J Med Chem (2021) 64: 14192-14216 [PMID:34605238]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.19 pKi 6438 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 4.71 pIC50 19315 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.65 pKi 2252 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.64 pIC50 2271 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells F 5.24 pKi 5780 nM Ki J Pharmacol Exp Ther (2002) 303: 323-332 [PMID:12235267]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 5.49 pKi 3200 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells F 4.34 pIC50 45600 nM IC50 Eur J Pharm Sci (2001) 12: 505-513 [PMID:11231118]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells F 4.65 pIC50 22500 nM IC50 Eur J Pharm Sci (2001) 12: 505-513 [PMID:11231118]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-CEM cells F 4.89 pEC50 12800 nM EC50 Anticancer Drugs (1996) 7: 568-578 [PMID:8862725]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells F 4.9 pKi 12700 nM Ki J Pharmacol Exp Ther (2002) 303: 323-332 [PMID:12235267]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells F 5.68 pKi 2100 nM Ki J Pharmacol Exp Ther (2002) 303: 323-332 [PMID:12235267]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum F 5.6 pIC50 2500 nM IC50 Antimicrob Agents Chemother (2007) 51: 2403-2411 [PMID:17485504]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.04 pIC50 9148 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 4.41 pKi 39167 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 4.06 pIC50 86167 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.99 pKi 1026 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.44 pIC50 3590 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.23 pKi 587 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.03 pIC50 923 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.67 pKi 212 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.39 pIC50 404 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.04 pKi 9026 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 4.71 pIC50 19441 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.91 pKi 1224 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.64 pIC50 2305 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 7.39 pKi 41 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 9 pKi 1 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 7.01 pIC50 97 nM IC50 DrugMatrix in vitro pharmacology data
Solute carrier organic anion transporter family member 1A4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin uptake in Xenopus laevis oocytes F 5.74 pKi 1800 nM Ki Endocrinology (2001) 142: 2005-2012 [PMID:11316767]
squalene monooxygenase/Squalene monooxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3592] [GtoPdb: 2433] [UniProtKB: Q14534]
ChEMBL Inhibitory activity against Trypanosoma cruzi microsomal squalene synthase B 4.92 pIC50 12000 nM IC50 J Med Chem (2006) 49: 892-899 [PMID:16451055]
squalene synthase /Squalene synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3338] [GtoPdb: 645] [UniProtKB: P37268]
ChEMBL Inhibitory activity against Trypanosoma cruzi glycosomal squalene synthase B 5.1 pIC50 8000 nM IC50 J Med Chem (2006) 49: 892-899 [PMID:16451055]
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
ChEMBL Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells B 6.19 pIC50 650 nM IC50 J Med Chem (2002) 45: 623-630 [PMID:11806713]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
ChEMBL Concentration required to inhibit 50% of binding of [125I]T3 to human Thyroid hormone receptor beta 1 in CHO-K1 cells B 6.22 pIC50 600 nM IC50 J Med Chem (2002) 45: 623-630 [PMID:11806713]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) B 6.09 pIC50 817 nM IC50 DrugMatrix in vitro pharmacology data
Kv1.7 in Human [GtoPdb: 544] [UniProtKB: Q96RP8]
GtoPdb - - 4.5 pKd - - - Eur J Hum Genet (2002) 10: 36-43 [PMID:11896454]
Nav1.5 in Rat [GtoPdb: 582] [UniProtKB: P15389]
GtoPdb - - 5.7 pIC50 - - - Circ Res (1989) 65: 477-82 [PMID:2546697]

ChEMBL data shown on this page come from version 35:

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]