nisoldipine [Ligand Id: 2524] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1726 (Nisoldipine, BAY-K-5552, Sular, Syscor mr 20, BAY K 5552, Syscor mr 10, Syscor mr 30)
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • This target only has 1 pki data point
  • 5.64
1 CHEMBL1726_lig_chart_1 Adenosine A2a receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • This target only has 1 pki data point
  • 5.4
2 CHEMBL1726_lig_chart_2 Adenosine A3 receptor Human
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  • CYP1A2/Cytochrome P450 1A2 in Human [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
  • This target only has 0 pki data point
  • 0
3 CHEMBL1726_lig_chart_3 Cytochrome P450 1A2 Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1726_lig_chart_4 HERG Human
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  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • This target only has 0 pki data point
  • 0
5 CHEMBL1726_lig_chart_5 P-glycoprotein 1 Human
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
  • This target only has 0 pki data point
  • 0
6 CHEMBL1726_lig_chart_6 Voltage-dependent L-type calcium channel subunit alpha-1C Guinea pig
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Cav1.2 in Mouse [GtoPdb: 529] [UniProtKB: Q01815]
  • This target only has 0 pki data point
  • 0
7 CHEMBL1726_lig_chart_7 Voltage-gated L-type calcium channel alpha-1C subunit HumanMouse
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  • Cav1.3 in Mouse [GtoPdb: 530] [UniProtKB: Q99246]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1726_lig_chart_8 Cav1.3 Mouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Journal of Applied Toxicology (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 Journal of Applied Toxicology (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 Journal of Applied Toxicology (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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]