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: CHEMBL452861 ((-)-propanolol, Propanolol) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 | Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
GtoPdb | - | - | 8.9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 525-32 [PMID:15060759]; Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; Pharmacol Res Perspect (2016) 4: e00250 [PMID:27588207] |
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 8.96 | pKi | 1.1 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 8.72 | pIC50 | 1.91 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells | B | 8.74 | pEC50 | 1.8 | nM | EC50 | J Nat Prod (2006) 69: 432-435 [PMID:16562853] |
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
ChEMBL | Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins | B | 9.27 | pKi | 0.54 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 9.61 | pKi | 0.24 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins | B | 9.11 | pIC50 | 0.78 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 9.45 | pIC50 | 0.35 | 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 | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.91 | pKi | 124 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.78 | pIC50 | 165 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells | F | 5.21 | pIC50 | 6100 | nM | IC50 | J Pharmacol Exp Ther (1999) 291: 1204-1209 [PMID:10565843] |
GtoPdb | - | - | 8.21 | pIC50 | 6.1 | nM | IC50 | J Pharmacol Exp Ther (1999) 291: 1204-9 [PMID:10565843] |
TLX/Nuclear receptor subfamily 2 group E member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961788] [GtoPdb: 615] [UniProtKB: Q9Y466] | ||||||||
ChEMBL | Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control | B | 4.14 | pEC50 | 72000 | nM | EC50 | J Med Chem (2021) 64: 8727-8738 [PMID:34115934] |
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
GtoPdb | - | - | 7.5 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 682-8 [PMID:9205951] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
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 | 6.94 | pKi | 115 | 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 | 7.15 | pKi | 71 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue using [3H]OH-DPAT as radioligand. | B | 7.26 | pKi | 55 | nM | Ki | J Med Chem (1989) 32: 859-863 [PMID:2539480] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.91 | pIC50 | 124 | 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 | 5.39 | pKi | 4100 | 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 | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand. | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1989) 32: 859-863 [PMID:2539480] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 6.27 | pKi | 538 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.73 | pIC50 | 1883 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Displacement of [3H]ketanserin from rat 5HT2A receptor expressed in mouse NIH3T3 cells | B | 5.09 | pKi | 8100 | nM | Ki | J Nat Prod (1997) 60: 651-653 [PMID:9214741] |
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 | 6.58 | pKi | 262 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.39 | pIC50 | 411 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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 | 5.85 | pKi | 1400 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 6.15 | pKi | 716 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.86 | pIC50 | 1368 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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 | 6.33 | pKi | 463 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6 | pIC50 | 998 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 6.18 | pKi | 659 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.91 | pIC50 | 1241 | 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 | 5.55 | pKi | 2801 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 5.18 | pIC50 | 6665 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
GtoPdb | - | - | 5.1 | pKi | - | - | - | FEBS Lett (1994) 355: 242-6 [PMID:7988681] |
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]