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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 |
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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 34:
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]