nifedipine [Ligand Id: 2514] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL193 (Nimodrel XL, Nife-Wolff, Hypolar XL 30, Adalat Cc, Neozipine XL, Nifedotard 20 MR, Procardia Xl, Afeditab Cr, Adalat LA 20, Nifopress Ret, Nimodrel MR 10, Adipine MR 10, Genalat 20 Ret, Nifopress MR, Adalat LA 30, Angiopine MR 20, BAY-A-1040, Procardia, Cardilate MR, Kentipine MR 20, Slofedipine XL 30, Tensipine MR 10, Coracten SR, Adalat IC, Genalat 10 Ret, Angiopine 40 LA, Kentipine MR 10, Nivaten Ret, Valni XL, Nifedipress MR 20, Calchan MR 20, Fortipine LA40, Valni 20 Ret, Nifensar Xl, Coracten XL, Hypolar Ret 10, Calanif, Adalat, Adipine XL, Adalat Ret, Adalat LA 60, Adipine MR 20, Vasad, Angiopine 5, Angiopine MR 10, Nifedipress MR 10, Adalate LP, Adanif XL, Tensipine MR 20, Hypolar Ret 20, Nimodrel MR 20, Coroday MR, Kentipine, Unipine XL, Adalat A.R., Calcilat, Calchan MR 10, Nifedipine, Slofedipine XL 60, Angiopine 10, Nifelease)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • 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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  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • glutathione-disulfide reductase/Glutathione reductase in Human [ChEMBL: CHEMBL2755] [GtoPdb: 2613] [UniProtKB: P00390]
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  • indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase 1 in Mouse [ChEMBL: CHEMBL1075294] [GtoPdb: 2829] [UniProtKB: P28776]
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  • indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5]
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  • myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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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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  • 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]
  • Voltage-gated L-type calcium channel alpha-1C subunit in Rabbit [ChEMBL: CHEMBL2830] [UniProtKB: P15381]
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • Cav1.3/Voltage-gated L-type calcium channel alpha-1D subunit in Human [ChEMBL: CHEMBL4138] [GtoPdb: 530] [UniProtKB: Q01668]
  • Cav1.3/Voltage-gated L-type calcium channel alpha-1D subunit in Rat [ChEMBL: CHEMBL4132] [GtoPdb: 530] [UniProtKB: P27732]
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  • Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
  • Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
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  • Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
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  • glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
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  • glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
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  • glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167]
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  • Cav1.1 in Rat [GtoPdb: 528] [UniProtKB: Q02485]
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  • Cav1.4 in Human [GtoPdb: 531] [UniProtKB: O60840]
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  • Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
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  • Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
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  • Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method B 5.4 pKi 4000 nM Ki Med Chem Res (2005) 14: 297-308
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 5.35 pKi 4492 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 5.11 pIC50 7701 nM IC50 DrugMatrix in vitro pharmacology data
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 pKi <10000 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
ChEMBL Binding affinity against adenosine A1 receptor in rat cerebral cortex membrane by radioligand binding assay using [3H](R)-PIA. B 5.54 pKi 2890 nM Ki J. Med. Chem. (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes B 5.54 pKi 2890 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 4.65 pKi 22200 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells B 4.65 pKi 22200 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
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 4.74 pKi 18200 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
ChEMBL Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes B 5 pKi <10000 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 pKi <10000 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
ChEMBL Inhibition of [125I]- AB-MECA binding to human Adenosine A3 receptors expressed in HEK cells B 5.08 pKi 8290 nM Ki J. Med. Chem. (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells B 5.08 pKi 8290 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.39 pKi 4078 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.14 pIC50 7214 nM IC50 DrugMatrix in vitro pharmacology data
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 4.82 pIC50 15101 nM IC50 DrugMatrix in vitro pharmacology data
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 4.51 pIC50 30700 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127]
ChEMBL Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 4.34 pIC50 45400 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1) B 6.07 pKi 847 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1) B 5.66 pIC50 2191 nM IC50 DrugMatrix in vitro pharmacology data
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 5.3 pKi 5011.87 nM Ki Med Chem Res (2005) 14: 297-308
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 5.92 pKi 1200 nM Ki Med Chem Res (2005) 14: 297-308
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 6.52 pIC50 300 nM IC50 DrugMatrix in vitro pharmacology data
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL Inhibition of CYP3A4 in human liver microsome B 4.96 pIC50 11000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1206-1213 [PMID:21256005]
glutathione-disulfide reductase/Glutathione reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2755] [GtoPdb: 2613] [UniProtKB: P00390]
ChEMBL Competitive inhibition of human erythrocyte Glutathione reductase using GSSG substrate by Lineweaver-Burk plot analysis B 4.76 pKi 17400 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 5398-5402 [PMID:21795044]
ChEMBL Inhibition of human erythrocyte Glutathione reductase B 4.63 pIC50 23400 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 5398-5402 [PMID:21795044]
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 4.3 pIC50 50118.72 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.3 pIC50 50118.72 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 4.3 pIC50 50118.72 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 4.3 pIC50 50118.72 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075294] [GtoPdb: 2829] [UniProtKB: P28776]
ChEMBL Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis B 4.34 pIC50 46000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 7641-7646 [PMID:23122865]
indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5]
ChEMBL Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis B 5.82 pIC50 1500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 7641-7646 [PMID:23122865]
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
ChEMBL Inhibition of MLCK (unknown origin) incubated for 15 mins using [gamma-32P]-ATP by scintillation counting method B 5.69 pIC50 2020 nM IC50 Bioorg. Med. Chem. (2015) 23: 6689-6713 [PMID:26385444]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 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 W2 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 3D7 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 GB4 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Potassium channel subfamily K member 2 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075183] [UniProtKB: Q8HY88]
ChEMBL Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents B 5.09 pIC50 8200 nM IC50 J. Med. Chem. (2016) 59: 5149-5157 [PMID:26588045]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.02 pKi 9572 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 4.74 pIC50 18273 nM IC50 DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 4.73 pIC50 18594 nM IC50 DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4028] [GtoPdb: 1353] [UniProtKB: P49430]
ChEMBL In vitro inhibition of thromboxane B2 production in rat whole blood. F 5 pIC50 >10000 nM IC50 J. Med. Chem. (1993) 36: 2964-2972 [PMID:8411014]
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 6.4 pEC50 400 nM EC50 J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305]
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 6.52 pIC50 300 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 6.59 pIC50 260 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of Calcium channel in Cavia porcellus albino (guinea pig) ileocecal SMC assessed as inhibition of 80 mM KCl-induced contraction B 7.16 pIC50 69 nM IC50 Med Chem Res (2012) 21: 284-292
ChEMBL Antagonist activity at Calcium channel in Cavia porcellus (guinea pig) ileal smooth muscle assessed as inhibition of 40 mM KCl-induced contraction compound pretreated for 15 min before KCl treatment B 7.3 pIC50 50 nM IC50 Med Chem Res (2009) 18: 112-126
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 7.3 pIC50 50 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Antagonist activity at Cavia porcellus albino (guinea pig) calcium channel assessed as inhibition of KCl-induced ileal longitudinal smooth muscle contraction B 8.59 pIC50 2.6 nM IC50 Med Chem Res (2012) 21: 2749-2761
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Displacement of [3H]nitrendipine from dihydropyridine receptor of guinea pig myocardial membranes B 9.4 pKd 0.4 nM Kd J. Med. Chem. (1995) 38: 119-129 [PMID:7837222]