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

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ChEMBL ligand: CHEMBL1484 (Nicardipine, Nicardipine (stn), Nicardipino, Perpidine)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A1 receptorpKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A2a receptorpKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A3 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
Created with Highcharts 10.3.3ValuesChart context menuATP-binding cassette sub-family G member 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Beta-lactamase AmpC in Escherichia coli [ChEMBL: CHEMBL2026] [UniProtKB: P00811]
Created with Highcharts 10.3.3ValuesChart context menuBeta-lactamase AmpCpKd Escherichia colipKi Escherichia colipIC50 Escherichia colipEC50 Escherichia coli012345Highcharts.com
  • Equilibrative nucleoside transporter 1 in Rat [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
Created with Highcharts 10.3.3ValuesChart context menuEquilibrative nucleoside transporter 1pKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • Malate dehydrogenase cytoplasmic in Human [ChEMBL: CHEMBL3560] [UniProtKB: P40925]
Created with Highcharts 10.3.3ValuesChart context menuMalate dehydrogenase cytoplasmicpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuP-glycoprotein 1pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 Mouse01234567Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuP-glycoprotein 3pKd MousepKi MousepIC50 MousepEC50 Mouse0123456Highcharts.com
  • Quinolone resistance protein norA in S.aureus [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7]
Created with Highcharts 10.3.3ValuesChart context menuQuinolone resistance protein norApKd S.aureuspKi S.aureuspIC50 S.aureuspEC50 S.aureus012345Highcharts.com
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
Created with Highcharts 10.3.3ValuesChart context menuTransient receptor potential cation channel subfamily A member 1pKd MousepKi MousepIC50 MousepEC50 Mouse01234567Highcharts.com
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
Created with Highcharts 10.3.3ValuesChart context menuVoltage-gated L-type calcium channel alpha-1C subunitpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • Kv1.4 in Rat [GtoPdb: 541] [UniProtKB: P15385]
Created with Highcharts 10.3.3ValuesChart context menuKv1.4pKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
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]
ChEMBL Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells assessed as reversal of BCRP-mediated mitoxantrone resistance and measured after 90 mins by FACSflow cytometry analysis B 5.32 pIC50 4800 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
Beta-lactamase AmpC in Escherichia coli (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 J Appl Toxicol (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 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 6.6 pIC50 250 nM IC50 J Appl Toxicol (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 35:

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]