nicardipine [Ligand Id: 2559] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1484 (Nicardipine, Nicardipine (stn), Perpidine) |
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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 (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 33:
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]
