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ChEMBL ligand: CHEMBL633 (Amiodarone, Cordarone, L-3428, Pacerone, SKF 33134-A) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
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]