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

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ChEMBL ligand: CHEMBL1726 (BAY K 5552, BAY-K-5552, Baymycard, Geomatrix 16e, Nisoldipin, Nisoldipine, Nisoldipine (stn), Nisoldipino, NSC-759106, Sular, Syscor mr 10, Syscor mr 20, Syscor mr 30)
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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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]
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  • Cav1.3 in Mouse [GtoPdb: 530] [UniProtKB: Q99246]
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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 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 34:

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]