nitrendipine [Ligand Id: 2334] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL475534 (BAY-E-5009, Baypress, BAY E 5009, Nitrendipine)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
There should be some charts here, you may need to enable JavaScript!
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Cav1.2 in Dog [GtoPdb: 529]
There should be some charts here, you may need to enable JavaScript!
  • KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.1 in Rat [GtoPdb: 528] [UniProtKB: Q02485]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.3 in Human [GtoPdb: 530] [UniProtKB: Q01668]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.4 in Human [GtoPdb: 531] [UniProtKB: O60840]
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
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes B 5.05 pKi 8960 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes B 4.64 pKi 23000 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells B 5.08 pKi 8300 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261]
ChEMBL DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.52 pIC50 3000 nM IC50 DrugMatrix in vitro pharmacology data
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.52 pIC50 300 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 5 pIC50 10000 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of hERG K channel F 5 pIC50 10000 nM IC50 Cardiovasc. Res. (2011) 91: 53-61 [PMID:21300721]
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 4.17 pIC50 68200 nM IC50 Eur. J. Pharm. Sci. (2002) 16: 159-165 [PMID:12128170]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Platelet activating factor receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
ChEMBL Tested for inhibition of [3H]PAF binding to rabbit Platelet activating factor receptor B 4.13 pKi 73310 nM Ki J. Med. Chem. (1990) 33: 3205-3210 [PMID:2175357]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
ChEMBL Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx F 5.42 pEC50 3800 nM EC50 J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of [3H]nitrendipine binding to L-type calcium channel in guinea pig ventricular myocardium membranes B 9.59 pKd 0.26 nM Kd J. Med. Chem. (1990) 33: 1510-1515 [PMID:2329573]
ChEMBL Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles B 9.6 pKi 0.25 nM Ki J. Med. Chem. (1987) 30: 690-695 [PMID:2435904]
Cav1.2 in Dog [GtoPdb: 529]
GtoPdb - - 9.4 pIC50 - - - Proc Natl Acad Sci USA (1984) 81: 6388-92 [PMID:6093100]
KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554]
GtoPdb - - 6.1 pKd - - - Proc Natl Acad Sci USA (2000) 97: 8151-6 [PMID:10884437]
GtoPdb - - 7.6 pIC50 - - - Am J Physiol (1998) 275: C848-56 [PMID:9730970]
Cav1.1 in Rat [GtoPdb: 528] [UniProtKB: Q02485]
GtoPdb - - 6 pIC50 - - - J Gen Physiol (1988) 91: 781-98 [PMID:2458429]
Cav1.3 in Human [GtoPdb: 530] [UniProtKB: Q01668]
GtoPdb Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells - 8.4 pIC50 3.59 nM IC50 Mol Pharmacol (2009) 75: 407-14 [PMID:19029287]
Cav1.4 in Human [GtoPdb: 531] [UniProtKB: O60840]
GtoPdb - - 6 pIC50 ~1000 nM IC50

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]