amlodipine [Ligand Id: 6981] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1491 (Amlodipine, Astudal 5, CKD-330 COMPONENT AMLODIPINE, HGP-0904, HGP0904, Istin, Norvas, Norvasc) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Binding affinity against human Alpha-1a adrenergic receptor | B | 5.63 | pKi | 2344 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2843-2848 [PMID:10522703] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity against human Alpha-1b adrenergic receptor | B | 5.1 | pKi | 7943 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2843-2848 [PMID:10522703] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Binding affinity against human Alpha-1d adrenergic receptor | B | 5.27 | pKi | 5370 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2843-2848 [PMID:10522703] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.65 | pKi | 226 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.22 | pIC50 | 602 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.58 | pKi | 261 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.74 | pIC50 | 1800 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.36 | pKi | 4387 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.26 | pIC50 | 5521 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells | F | 4.66 | pIC50 | 22000 | nM | IC50 | Pharm Res (2000) 17: 1189-1197 [PMID:11145223] |
| K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069] | ||||||||
| ChEMBL | Inhibition of TREK-1 (unknown origin) | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| Potassium channel subfamily K member 2 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075183] [UniProtKB: Q8HY88] | ||||||||
| ChEMBL | Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2016) 59: 5149-5157 [PMID:26588045] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.87 | pKi | 1346 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.54 | pIC50 | 2898 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
| ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 6.24 | pIC50 | 570 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| 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 | 5.38 | pIC50 | 4200 | 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 | 5.92 | pIC50 | 1200 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| Cav1.2 in Rabbit [GtoPdb: 529] | ||||||||
| GtoPdb | Determined in vascular smooth muscle. | - | 9.3 | pIC50 | - | - | - | Br J Pharmacol (1993) 109: 120-5 [PMID:8388295] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002] | ||||||||
| ChEMBL | Binding affinity against rat L-type calcium channel | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2843-2848 [PMID:10522703] |
| Cav1.3 in Human [GtoPdb: 530] [UniProtKB: Q01668] | ||||||||
| GtoPdb | Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells | - | 7.2 | pIC50 | 60.1 | nM | IC50 | Mol Pharmacol (2009) 75: 407-14 [PMID:19029287] |
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]
