amlodipine [Ligand Id: 6981] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1491 (Amlodipine, Amlodipino, Astudal 5, CKD-330 COMPONENT AMLODIPINE, HGP-0904, HGP0904, Istin, Norvas, Norvasc)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1b adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1d adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2c adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuDopamine transporterpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuP-glycoprotein 1pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
  • Potassium channel subfamily K member 2 in Bovine [ChEMBL: CHEMBL1075183] [UniProtKB: Q8HY88]
Created with Highcharts 10.3.3ValuesChart context menuPotassium channel subfamily K member 2pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 Bovine02468Highcharts.com
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 6 (5-HT6) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
Created with Highcharts 10.3.3ValuesChart context menuVoltage-dependent L-type calcium channel subunit alpha-1CpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig01234567Highcharts.com
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Cav1.2 in Rabbit [GtoPdb: 529]
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
Created with Highcharts 10.3.3ValuesChart context menuVoltage-gated L-type calcium channel alpha-1C subunitpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RabbitpKi RabbitpIC50 RabbitpEC50 RabbitpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • Cav1.3 in Human [GtoPdb: 530] [UniProtKB: Q01668]
Created with Highcharts 10.3.3ValuesChart context menuCav1.3pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
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 35:

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]