nicardipine [Ligand Id: 2559] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1484 (Nicardipine)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
  • This target only has 1 pki data point
  • 4.71
1 CHEMBL1484_lig_chart_1 Adenosine A1 receptor Rat
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
  • This target only has 1 pki data point
  • 4.2
2 CHEMBL1484_lig_chart_2 Adenosine A2a receptor Rat
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
  • 4.96
3 CHEMBL1484_lig_chart_3 Adenosine A3 receptor HumanRat
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  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1484_lig_chart_4 ATP-binding cassette sub-family G member 2 Human
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  • Beta-lactamase AmpC in Escherichia coli K-12 [ChEMBL: CHEMBL2026] [UniProtKB: P00811]
  • This target only has 0 pki data point
  • 0
5 CHEMBL1484_lig_chart_5 Beta-lactamase AmpC Escherichia coli K-12
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  • Equilibrative nucleoside transporter 1 in Rat [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
  • This target only has 1 pki data point
  • 5.27
6 CHEMBL1484_lig_chart_6 Equilibrative nucleoside transporter 1 Rat
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  • Malate dehydrogenase cytoplasmic in Human [ChEMBL: CHEMBL3560] [UniProtKB: P40925]
  • This target only has 0 pki data point
  • 0
7 CHEMBL1484_lig_chart_7 Malate dehydrogenase cytoplasmic Human
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  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1484_lig_chart_8 P-glycoprotein 1 HumanMouse
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  • ABCB1/P-glycoprotein 3 in Mouse [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
  • This target only has 0 pki data point
  • 0
9 CHEMBL1484_lig_chart_9 P-glycoprotein 3 Mouse
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  • Quinolone resistance protein norA in S.aureus [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7]
  • This target only has 0 pki data point
  • 0
10 CHEMBL1484_lig_chart_10 Quinolone resistance protein norA S.aureus
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
  • This target only has 0 pki data point
  • 0
11 CHEMBL1484_lig_chart_11 Transient receptor potential cation channel subfamily A member 1 Mouse
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • This target only has 0 pki data point
  • 0
12 CHEMBL1484_lig_chart_12 Voltage-gated L-type calcium channel alpha-1C subunit Human
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  • Kv1.4 in Rat [GtoPdb: 541] [UniProtKB: P15385]
  • This target only has 0 pki data point
  • 0
13 CHEMBL1484_lig_chart_13 Kv1.4 Rat
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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 4.71 pKi 19600 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 4.2 pKi 63800 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 5.49 pKi 3250 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
GtoPdb - - 5.5 pKi - - - J Med Chem (1996) 39: 2980-9 [PMID:8709132]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Binding affinity against rat Adenosine A3 receptor from CHO cells B 4.96 pKi 11000 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay B 4.78 pIC50 16595.87 nM IC50 Bioorg. Med. Chem. (2008) 16: 8224-8236 [PMID:18678495]
Beta-lactamase AmpC in Escherichia coli K-12 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2026] [UniProtKB: P00811]
ChEMBL Compound was tested for the inhibition of beta-lactamase B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2003) 46: 4477-4486 [PMID:14521410]
ChEMBL Inhibitory activity against Amp C beta-Lactamase B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2003) 46: 4265-4272 [PMID:13678405]
ChEMBL Inhibitory activity against Beta-lactamase from DMSO stock was determined B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2003) 46: 4265-4272 [PMID:13678405]
Equilibrative nucleoside transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
ChEMBL Ability to displace radioligand from Na+ independent Adenosine transporter in rat B 5.27 pKi 5360 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
Malate dehydrogenase cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3560] [UniProtKB: P40925]
ChEMBL Inhibition of malate dehydrogenase (MDH) B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (2003) 46: 4477-4486 [PMID:14521410]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 4.59 pIC50 >25800 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells F 4.76 pIC50 17500 nM IC50 Pharm. Res. (2000) 17: 1189-1197 [PMID:11145223]
ChEMBL TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells F 4.84 pIC50 14600 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells F 4.93 pIC50 11700 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells F 5.15 pIC50 7100 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells F 5.18 pIC50 6600 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.25 pIC50 5600 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL Inhibition of P-glycoprotein by Hoechst assay B 5.29 pIC50 5128.61 nM IC50 Bioorg. Med. Chem. (2007) 15: 7470-7479 [PMID:17890094]
ChEMBL Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay B 5.32 pIC50 4786.3 nM IC50 Bioorg. Med. Chem. (2007) 15: 7470-7479 [PMID:17890094]
ChEMBL Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay B 5.32 pIC50 4786.3 nM IC50 Bioorg. Med. Chem. (2008) 16: 8224-8236 [PMID:18678495]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells F 5.34 pIC50 4540 nM IC50 Eur. J. Pharm. Sci. (2002) 16: 159-165 [PMID:12128170]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.49 pIC50 3200 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.64 pIC50 2300 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 5.64 pIC50 2300 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 6.02 pIC50 950 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.1 pIC50 8000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 5.1 pIC50 8000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.6 pIC50 2500 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 5.6 pIC50 2500 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
Quinolone resistance protein norA in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7]
ChEMBL Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux after 5 mins by fluorometric method B 4.64 pIC50 22800 nM IC50 J Med Chem (2017) 60: 1598-1604 [PMID:28117588]
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 6.3 pEC50 500 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 L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit F 4.62 pIC50 24100 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit F 5.02 pIC50 9600 nM IC50 Journal of Applied Toxicology (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 6.6 pIC50 250 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
Kv1.4 in Rat [GtoPdb: 541] [UniProtKB: P15385]
GtoPdb - - 6.1 pIC50 - - - Br J Pharmacol (2003) 139: 533-44 [PMID:12788813]

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]