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ChEMBL ligand: CHEMBL1726 (BAY K 5552, BAY-K-5552, Baymycard, Geomatrix 16e, Nisoldipin, Nisoldipine, Nisoldipine (stn), NSC-759106, Sular, Syscor mr 10, Syscor mr 20, Syscor mr 30) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.64 | pKi | 2278 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.39 | pIC50 | 4058 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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 | 5.4 | pKi | 4024 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.15 | pIC50 | 7120 | nM | IC50 | DrugMatrix in vitro pharmacology data |
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177] | ||||||||
ChEMBL | DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6 | pIC50 | 1000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibitory concentration against IKr potassium channel | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells | F | 4.36 | pIC50 | 44100 | nM | IC50 | Eur J Pharm Sci (2002) 16: 159-165 [PMID:12128170] |
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 6.14 | pIC50 | 730 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 7.1 | pIC50 | 80 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
GtoPdb | - | - | 7.1 | pIC50 | - | - | - | Cell (2004) 119: 19-31 [PMID:15454078] |
ChEMBL | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit | F | 8.52 | pIC50 | 3 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
Cav1.2 in Mouse [GtoPdb: 529] [UniProtKB: Q01815] | ||||||||
GtoPdb | - | - | 8 | pIC50 | - | - | - | J Biol Chem (2000) 275: 39193-9 [PMID:10973973] |
Cav1.3 in Mouse [GtoPdb: 530] [UniProtKB: Q99246] | ||||||||
GtoPdb | - | - | 7 | pIC50 | - | - | - | J Biol Chem (2003) 278: 40837-41 [PMID:12900400] |
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]