nitrendipine [Ligand Id: 2334] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL475534 (BAY E 5009, BAY-E-5009, Bayotensin, Baypress, Deiten, Nidrel, Nitrendipine, Nitrendipino, Nitrepin, NSC-758466) |
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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 | 5.05 | pKi | 8960 | 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 | 4.64 | pKi | 23000 | 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 | 5.08 | pKi | 8300 | 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 (unknown origin) expressed in human MCF7/MX cells mediated mitoxantrone efflux assessed as intracellular mitoxantrone level and measured after 30 mins by FACSflow cytometry analysis | B | 4.68 | pIC50 | 21100 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 5.52 | pIC50 | 3000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6.52 | pIC50 | 300 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5 | pIC50 | 10000 | 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 | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
| ChEMBL | Inhibition of human ERG | B | 5 | pIC50 | 10000 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibition of hERG K channel | F | 5 | pIC50 | 10000 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells | F | 4.17 | pIC50 | 68200 | nM | IC50 | Eur J Pharm Sci (2002) 16: 159-165 [PMID:12128170] |
| phosphodiesterase 1C/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 | 5.73 | pIC50 | 1850 | nM | IC50 | J Med Chem (2022) 65: 8444-8455 [PMID:35666471] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 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 GB4 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 Dd2 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 HB3 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 W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | 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 | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Platelet activating factor receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5136] [UniProtKB: P21556] | ||||||||
| ChEMBL | Tested for inhibition of [3H]PAF binding to rabbit Platelet activating factor receptor | B | 4.13 | pKi | 73310 | nM | Ki | J Med Chem (1990) 33: 3205-3210 [PMID:2175357] |
| 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 | 5.42 | pEC50 | 3800 | 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 [3H]nitrendipine binding to L-type calcium channel in guinea pig ventricular myocardium membranes | B | 9.59 | pKd | 0.26 | nM | Kd | J Med Chem (1990) 33: 1510-1515 [PMID:2329573] |
| ChEMBL | Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (1987) 30: 690-695 [PMID:2435904] |
| Cav1.2 in Dog [GtoPdb: 529] | ||||||||
| GtoPdb | - | - | 9.4 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1984) 81: 6388-92 [PMID:6093100] |
| KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554] | ||||||||
| GtoPdb | - | - | 6.1 | pKd | - | - | - | Proc Natl Acad Sci USA (2000) 97: 8151-6 [PMID:10884437] |
| GtoPdb | - | - | 7.6 | pIC50 | - | - | - | Am J Physiol (1998) 275: C848-56 [PMID:9730970] |
| Cav1.1 in Rat [GtoPdb: 528] [UniProtKB: Q02485] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | - | - | - | J Gen Physiol (1988) 91: 781-98 [PMID:2458429] |
| Cav1.3 in Human [GtoPdb: 530] [UniProtKB: Q01668] | ||||||||
| GtoPdb | Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells | - | 8.4 | pIC50 | 3.59 | nM | IC50 | Mol Pharmacol (2009) 75: 407-14 [PMID:19029287] |
| Cav1.4 in Human [GtoPdb: 531] [UniProtKB: O60840] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | ~1000 | nM | IC50 | |
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]
