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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 |
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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 | 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 | 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] |
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]