ChEMBL ligand: CHEMBL481 (Biotecan, Irinotecan, NSC-728073)
Acetylcholinesterase in Torpedo californica [ChEMBL: CHEMBL4780] [UniProtKB: P04058] acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] There should be some charts here, you may need to enable JavaScript!
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] There should be some charts here, you may need to enable JavaScript!
MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] There should be some charts here, you may need to enable JavaScript!
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] There should be some charts here, you may need to enable JavaScript!
MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] There should be some charts here, you may need to enable JavaScript!
M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] There should be some charts here, you may need to enable JavaScript!
Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] There should be some charts here, you may need to enable JavaScript!
Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] There should be some charts here, you may need to enable JavaScript!
Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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 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]