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ChEMBL ligand: CHEMBL481 (Biotecan, Camptosar, Irinotecan, NSC-728073) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Acetylcholinesterase in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4780] [UniProtKB: P04058] | ||||||||
ChEMBL | Inhibition of Torpedo californica AChE | B | 7.58 | pKi | 26.4 | nM | Ki | J Med Chem (2008) 51: 3154-3170 [PMID:18479118] |
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
ChEMBL | Inhibition of human AChE | B | 7.3 | pKi | 50.5 | nM | Ki | J Med Chem (2008) 51: 3154-3170 [PMID:18479118] |
ChEMBL | DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) | B | 5.74 | pIC50 | 1827 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.34 | pKi | 461 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.5 | pIC50 | 3171 | nM | IC50 | DrugMatrix in vitro pharmacology data |
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
ChEMBL | DRUGMATRIX: Peptidase, Matrix Metalloprotease-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) | B | 5.22 | pIC50 | 6060 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.1 | pIC50 | 7900 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | B | 5.37 | pIC50 | 4300 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.1 | pIC50 | 78600 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay | B | 5.1 | pIC50 | 7900 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
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 | 6.66 | pKi | 217 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.81 | pIC50 | 1556 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
ChEMBL | Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.68 | pIC50 | 20800 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
ChEMBL | Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.13 | pIC50 | 74600 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
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]