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, 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] |
| 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] |
| 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 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]
