pindolol [Ligand Id: 91] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL500 (LB-46, Visken, Prinodolol, Pindolol, Betadren)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis F 5 pKd <10000 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells B 8.58 pKd 2.63 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis F 8.62 pKd 2.4 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 9.27 pKi 0.53 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity at human adrenergic beta-1 receptor B 9.28 pKi 0.52 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5600-5604 [PMID:17804228]
GtoPdb - - 9.3 pKi 0.52 nM Ki Bioorg Med Chem Lett (2007) 17: 5600-4 [PMID:17804228]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 9.04 pIC50 0.92 nM IC50 DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis F 9.18 pKd 0.66 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells B 9.27 pKd 0.54 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Binding affinity at human adrenergic beta2 receptor B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5600-5604 [PMID:17804228]
GtoPdb - - 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (2007) 17: 5600-4 [PMID:17804228]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 9.42 pKi 0.38 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 9.26 pIC50 0.55 nM IC50 DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis F 6 pKd <1000 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells B 6.78 pKd 165.96 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 7.18 pKi 66 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 7.06 pIC50 88 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to 5HT1A receptor B 7.2 pKd 63.1 nM Kd J. Med. Chem. (2009) 52: 6107-6125 [PMID:19754201]
ChEMBL Inhibition constant against 5-hydroxytryptamine 1A receptor B 6.96 pKi 110 nM Ki J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as inhibition of 5-HT-stimulated [35S]GTP-gamma-S binding F 7.09 pKi 81.1 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5600-5604 [PMID:17804228]
ChEMBL Displacement of specific [3H]- 5-HT binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells B 7.62 pKi 24 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3243-3248 [PMID:10576696]
ChEMBL Displacement of [3H]DPAT from human 5HT1A receptor B 7.65 pKi 22.4 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5600-5604 [PMID:17804228]
GtoPdb - - 8.1 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]
ChEMBL Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells B 7.57 pEC50 27 nM EC50 Bioorg. Med. Chem. Lett. (1999) 9: 3243-3248 [PMID:10576696]
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 7.57 pKi 27 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 7.66 pKi 21.88 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. B 7.7 pKi 20 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 7.32 pIC50 48 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptor F 5 pKi >10000 nM Ki J. Med. Chem. (1997) 40: 4415-4419 [PMID:9435911]
ChEMBL Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptor F 5.59 pKi 2600 nM Ki J. Med. Chem. (1997) 40: 4415-4419 [PMID:9435911]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. B 7.1 pKi 80 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. B 4.27 pKi 54000 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Displacement of specific [3H]- citalopram binding to 5-HT uptake site in rat whole cortex B 5.15 pKi >7000 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3243-3248 [PMID:10576696]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
GtoPdb - - 5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 5.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
GtoPdb - - 5.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]