labetalol [Ligand Id: 7207] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL429 (AH-5158A FREE BASE, Ibidomide, Labetalol, Normodyne, Normozide, SCH-15719W FREE BASE, Trandate)
  • α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
Created with Highcharts 10.3.3ValuesChart context menuα1A-adrenoceptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1b adrenergic receptorpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.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 Human02468Highcharts.com
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
Created with Highcharts 10.3.3ValuesChart context menuBeta-1 adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig0246810Highcharts.com
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
Created with Highcharts 10.3.3ValuesChart context menuBeta-2 adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig0246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCytochrome P450 2D6pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuDopamine transporterpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
Created with Highcharts 10.3.3ValuesChart context menuNorepinephrine transporterpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 1a (5-HT1a) receptorpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 2b (5-HT2b) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
Created with Highcharts 10.3.3ValuesChart context menuSigma opioid receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
GtoPdb - - 7.3 pKi - - - Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
GtoPdb - - 7.9 pIC50 - - - Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.64 pKi 23 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.24 pIC50 57 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.49 pKi 323 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.23 pIC50 583 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.59 pKi 256 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.6 pKi - - - National Toxicology Program: Dept of Health and Human Services.. DrugMatrix;
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.28 pIC50 521 nM IC50 DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
GtoPdb - - 8.2 pKi - - - Br J Pharmacol (2005) 144: 317-22 [PMID:15655528];
Mol Pharmacol (2003) 64: 1357-69 [PMID:14645666];
National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 8.23 pKi 5.84 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 8 pIC50 10 nM IC50 DrugMatrix in vitro pharmacology data
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor. F 7.5 pKd 31.62 nM Kd J Med Chem (1986) 29: 1009-1015 [PMID:3012084]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.96 pKi 11 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.96 pKi 11 nM Ki Br J Pharmacol (2005) 144: 317-22 [PMID:15655528];
National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.8 pIC50 16 nM IC50 DrugMatrix in vitro pharmacology data
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
ChEMBL The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor. F 7.4 pKd 39.81 nM Kd J Med Chem (1986) 29: 1009-1015 [PMID:3012084]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.1 pIC50 800 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 5.89 pKi 1277 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.79 pIC50 1607 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.48 pKi 3326 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.47 pIC50 3354 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.65 pKi 225 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.41 pIC50 393 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.71 pKi 1933 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.52 pIC50 3037 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.12 pKi 763 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.74 pIC50 1815 nM IC50 DrugMatrix in vitro pharmacology data

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]