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

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ChEMBL ligand: CHEMBL475534 (BAY E 5009, BAY-E-5009, Bayotensin, Baypress, Deiten, Nidrel, Nitrendipine, Nitrepin, NSC-758466)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
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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 Dog [GtoPdb: 529]
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  • KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554]
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  • Cav1.1 in Rat [GtoPdb: 528] [UniProtKB: Q02485]
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  • Cav1.3 in Human [GtoPdb: 530] [UniProtKB: Q01668]
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  • Cav1.4 in Human [GtoPdb: 531] [UniProtKB: O60840]
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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 32:

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]