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

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ChEMBL ligand: CHEMBL193 (Slofedipine xl 30, Angiopine 10, BAY-A-1040, Nivaten ret, Valni xl, Hypolar ret 20, Nifedipress mr 20, Adipine xl, Genalat 10 ret, Nimodrel mr 20, Nifensar xl, Fortipine la40, Nifedipine hydrochloride, Procardia xl, Adalat cc, Slofedipine xl 60, Kentipine mr 20, Adalat la 20, Kentipine mr 10, Nifelease, Calanif, Kentipine, Angiopine 40 la, Nifedipinum, Nifopress mr, BAY A 1040, Nifedipine, Nife-wolff, Adalat ret, Adipine mr 20, Nifedotard 20 mr, Tensipine mr 10, Hypolar ret 10, Adipine mr 10, Adalate lp, Angiopine mr 10, Genalat 20 ret, Angiopine 5, Adalat, Cardilate mr, Nimodrel xl, Nimodrel mr 10, Procardia, Calchan mr 10, Unipine xl, Adalat la 30, Calchan mr 20, Vasad, Coracten, Tensipine mr 20, Valni 20 ret, Adalat la 60, Adalat a.r., Nifedipino, Nifedipress mr 10, Coroday mr, Hypolar xl 30, Angiopine mr 20, Neozipine xl, Coracten sr, Coracten xl, Nifedipine slow release, Nifopress ret, Afeditab cr, Calcilat, NSC-757242, Adalat ic, Adanif xl)
  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • A1 receptor/Adenosine receptor A1 in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine receptor A1 in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine receptor A2a in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine receptor A2a in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine receptor A3 in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • phosphodiesterase 1C/Dual specificity calcium/calmodulin-dependent 3`,5`-cyclic nucleotide phosphodiesterase 1C in Human [ChEMBL: CHEMBL4619] [GtoPdb: 1296] [UniProtKB: Q14123]
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  • glutathione-disulfide reductase/Glutathione reductase, mitochondrial 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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  • Polyunsaturated fatty acid lipoxygenase ALOX15 in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • Kv1.1/Potassium voltage-gated channel subfamily A member 1 in Human [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
  • Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
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  • Kv1.5/Potassium voltage-gated channel subfamily A member 5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
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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-dependent L-type calcium channel subunit alpha-1C in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Voltage-dependent L-type calcium channel subunit alpha-1C in Rabbit [ChEMBL: CHEMBL2830] [UniProtKB: P15381]
  • Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Cav1.3/Voltage-dependent L-type calcium channel subunit alpha-1D in Human [ChEMBL: CHEMBL4138] [GtoPdb: 530] [UniProtKB: Q01668]
  • Cav1.3/Voltage-dependent L-type calcium channel subunit alpha-1D in Rat [ChEMBL: CHEMBL4132] [GtoPdb: 530] [UniProtKB: P27732]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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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
5-HT2C receptor/5-hydroxytryptamine receptor 2C 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
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 receptor A1 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 receptor A1 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 receptor A2a 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 receptor A2a 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 receptor A3 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
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]
ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of human ABCG2 expressed in human HEK293 cells mediated pheophorbide A efflux assessed as intracellular pheophorbide A accumulation for 45 mins by FACSort flow cytometry B 4.3 pIC50 50500 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
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]
phosphodiesterase 1C/Dual specificity calcium/calmodulin-dependent 3`,5`-cyclic nucleotide phosphodiesterase 1C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4619] [GtoPdb: 1296] [UniProtKB: Q14123]
ChEMBL Inhibition of PDE1C (147 to 531 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 8444-8455 [PMID:35666471]
glutathione-disulfide reductase/Glutathione reductase, mitochondrial 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]
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]
Polyunsaturated fatty acid lipoxygenase ALOX15 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
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]
Kv1.1/Potassium voltage-gated channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
ChEMBL Inhibition of Kv1.1 (unknown origin) B 4.02 pIC50 96000 nM IC50 J Med Chem (2017) 60: 2245-2256 [PMID:28225274]
Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
GtoPdb - - 4 pIC50 - - - Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.5/Potassium voltage-gated channel subfamily A member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
GtoPdb - - 4.1 pKd - - - Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
ChEMBL Inhibition of human Kv1.5 channel expressed in mouse L929 cells by EP voltage clamp technique B 5.21 pIC50 6100 nM IC50 Bioorg Med Chem Lett (2008) 18: 6381-6385 [PMID:19004630]
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]
Translocator protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
ChEMBL Inhibition of rat TSPO B 9.3 pIC50 0.5 nM IC50 Eur J Med Chem (2024) 267: 116117-116117 [PMID:38295689]
Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C 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]
ChEMBL Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles B 9 pKi 1 nM Ki J Med Chem (1987) 30: 690-695 [PMID:2435904]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 7.26 pIC50 55 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit F 7.3 pIC50 50 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 7.66 pIC50 22 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Voltage-dependent L-type calcium channel subunit alpha-1C in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2830] [UniProtKB: P15381]
ChEMBL Blockade of calcium-evoked contractions in depolarized aortic strips F 8.54 pIC50 2.9 nM IC50 J Med Chem (1992) 35: 2407-2414 [PMID:1377748]
ChEMBL Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle. B 9 pIC50 1 nM IC50 J Med Chem (1988) 31: 2221-2227 [PMID:3184128]
Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of [3H](+)-PN200-110 binding to L-type calcium channel 1,4-DHP binding site of rat ventricular myocytes B 8.46 pKi 3.5 nM Ki J Med Chem (1993) 36: 3743-3745 [PMID:8246246]
GtoPdb guinea pig, human stem cell-derived cardiomyocytes - 8.7 pIC50 2 nM IC50 Am J Physiol Heart Circ Physiol (2000) 279: H2259-68 [PMID:11045961];
J Cardiovasc Pharmacol (1993) 22: 768-75 [PMID:7506331]
ChEMBL Inhibition of rat Cav1.2 channel in rat mesenteric artery assessed as relaxation of 70 mM K+ induced contraction B 8.85 pIC50 1.42 nM IC50 J Med Chem (2014) 57: 4313-4323 [PMID:24754640]
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 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 6.59 pIC50 260 nM IC50 J Appl Toxicol (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 J Appl Toxicol (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
Cav1.3/Voltage-dependent L-type calcium channel subunit alpha-1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4138] [GtoPdb: 530] [UniProtKB: Q01668]
ChEMBL Inhibition of human Cav1.3 channel in human SH-SY5Y cells assessed as 70 mM K+ induced calcium elevation compound treated 15 mins before stimulus by Fluo-4/AM assay B 5.87 pIC50 1350 nM IC50 J Med Chem (2014) 57: 4313-4323 [PMID:24754640]
GtoPdb Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells - 7.7 pIC50 20.1 nM IC50 Mol Pharmacol (2009) 75: 407-14 [PMID:19029287]
Cav1.3/Voltage-dependent L-type calcium channel subunit alpha-1D in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4132] [GtoPdb: 530] [UniProtKB: P27732]
ChEMBL Binding affinity for L-type [Ca2+] channels was measured through displacement of [3H]nitrendipine on rat cortex homogenates. B 8.92 pKi 1.2 nM Ki J Med Chem (1998) 41: 5393-5401 [PMID:9876109]
ChEMBL Inhibitory concentration for L-type [Ca2+] channels was measured through displacement of [3H]nitrendipine on rat cortex homogenates. B 8.57 pIC50 2.7 nM IC50 J Med Chem (1998) 41: 5393-5401 [PMID:9876109]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
GtoPdb - - 5.5 pIC50 3300 nM IC50
glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
GtoPdb - - 4.5 pIC50 29200 nM IC50
glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167]
GtoPdb - - 4.9 pIC50 11400 nM IC50
GtoPdb - - 5.9 pIC50 1200 nM IC50
Cav1.1 in Rat [GtoPdb: 528] [UniProtKB: Q02485]
GtoPdb - - 6.3 pIC50 - - - J Physiol (Lond.) (1987) 393: 595-617 [PMID:2451745]
Cav1.4 in Human [GtoPdb: 531] [UniProtKB: O60840]
GtoPdb - - 6 pIC50 - - - J Neurosci (2004) 24: 1707-18 [PMID:14973233]
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
GtoPdb - - 4.7 pKd 18000 nM Kd Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
GtoPdb - - 4.9 pIC50 - - - J Biol Chem (1998) 273: 5851-7 [PMID:9488722]
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
GtoPdb - - 3.9 pIC50 - - - Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]

ChEMBL data shown on this page come from version 36:

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]