pindolol [Ligand Id: 91] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL500 (Apo-pindol, Betadren, Betapindol, Blocklin-l, Calvisken, Carvisken, Decreten, Dl-lb-46, Dl-pindolol, Durapindol, Glauco-visken, LB-46, NSC-757276, Pectobloc, Pinbetol, Pindolol, Prinodolol, Pynastin, (rs)-pindolol, Visken) |
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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 | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Bioorg Med Chem Lett (2007) 17: 5600-4 [PMID:17804228] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 525-32 [PMID:15060759]; Mol Pharmacol (2003) 64: 1357-69 [PMID:14645666]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 | PDSP Secondary Binding target: ADRB2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 8.31 | pKi | 4.91 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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 | - | - | - | Bioorg Med Chem Lett (2007) 17: 5600-4 [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 | Binding affinity to human beta 2 adrenergic receptor assessed as inhibition constant | B | 9.49 | pKi | 0.32 | nM | Ki | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2 | F | 8.66 | pIC50 | 2.19 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 |
| GtoPdb | - | - | 7.4 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | PDSP Secondary Binding target: DRD3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6 | pKi | 994.49 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | PDSP Secondary Binding target: DRD4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.78 | pKi | 1661.88 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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 | PDSP Secondary Binding target: HTR1A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.81 | pKi | 153.64 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR5A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.15 | pKi | 7048.55 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TMEM97 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.48 | pKi | 3315.13 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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 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]
