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 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]
