clonidine [Ligand Id: 516] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL134 (Catapres, Catapres-tts-1, Catapres-tts-2, Catapres-tts-3, Catarpres-tts, Clonidine, Clonidine extended release, Clorpres, Combipres, Duraclon, Nexiclon xr, ST-155-BS, ST-155BS) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin | B | 6.01 | pKi | 977.24 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| ChEMBL | Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin | B | 6.29 | pKi | 512.86 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay | F | 7.05 | pEC50 | 89 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta. | B | 6.59 | pKd | 257.04 | nM | Kd | J Med Chem (1991) 34: 3197-3204 [PMID:1956038] |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.82 | pKi | 151 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.43 | pIC50 | 372 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Alpha-1B adrenergic receptor in Cricetulus griseus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988626] [UniProtKB: G3HDX1] | ||||||||
| ChEMBL | Agonist activity at hamster recombinant alpha-1B receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay | F | 7.08 | pEC50 | 83 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| 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 | 5.99 | pKi | 1023 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.73 | pIC50 | 1848 | 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] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.23 | pKi | 595 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.92 | pIC50 | 1210 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Mol Pharmacol (1994) 46: 929-36 [PMID:7969082] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Binding affinity towards Alpha-2A adrenergic receptor | B | 6.07 | pKi | 853 | nM | Ki | J Med Chem (2000) 43: 765-768 [PMID:10715142] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.98 | pKi | 105 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter | B | 8.06 | pKi | 8.71 | nM | Ki | Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139] |
| ChEMBL | Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| ChEMBL | Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (1996) 39: 3533-3538 [PMID:8784451] |
| ChEMBL | Binding affinity for human Alpha-2A adrenergic receptor | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
Biochim Biophys Acta (1998) 1448: 135-46 [PMID:9824686]; Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]; Eur J Pharmacol (1998) 355: 275-9 [PMID:9760042]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.55 | pIC50 | 280 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 8.2 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 6.4 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting | F | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem (2012) 20: 108-116 [PMID:22172308] |
| ChEMBL | Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.55 | pEC50 | 28 | nM | EC50 | Bioorg Med Chem (2011) 19: 321-329 [PMID:21129985] |
| GtoPdb | GTPγs binding | - | 7.6 | pEC50 | - | - | - | Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427] |
| ChEMBL | Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay | F | 8 | pEC50 | 10 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| ChEMBL | Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry | F | 8.08 | pEC50 | 8.32 | nM | EC50 | J Med Chem (2010) 53: 7825-7835 [PMID:20925410] |
| ChEMBL | Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate | F | 8.09 | pEC50 | 8.13 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| GtoPdb | increased ERK1/2 phosphorylation | - | 9 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838] | ||||||||
| ChEMBL | Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1989) 32: 720-727 [PMID:2537429] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand | B | 6.07 | pKi | 853 | nM | Ki | J Med Chem (2000) 43: 1423-1426 [PMID:10753480] |
| ChEMBL | Binding affinity towards alpha-2D adrenergic receptor | B | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (2000) 43: 765-768 [PMID:10715142] |
| ChEMBL | In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine | B | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (2000) 43: 1423-1426 [PMID:10753480] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.42 | pKi | 38 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]RX821001 from human alpha2B adrenoceptor expressed in CHO cells after 60 mins by gamma counter | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139] |
| ChEMBL | Binding affinity towards human Alpha-2B adrenergic receptor by the displacement of [3H]rauwolscine | B | 8.21 | pKi | 6.17 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| GtoPdb | - | - | 9.5 | pKi | - | - | - |
Biochim Biophys Acta (1998) 1448: 135-46 [PMID:9824686]; Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]; Eur J Pharmacol (1998) 355: 275-9 [PMID:9760042]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.08 | pIC50 | 83 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 8.6 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry | F | 5.93 | pEC50 | 1174.9 | nM | EC50 | J Med Chem (2010) 53: 7825-7835 [PMID:20925410] |
| ChEMBL | Agonistic activity towards human Alpha-2B adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate | F | 6.78 | pEC50 | 165.96 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| GtoPdb | cAMP generation | - | 7.4 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328] | ||||||||
| ChEMBL | in vitro alpha-2B adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2000) 43: 1423-1426 [PMID:10753480] |
| ChEMBL | Compound was tested in vitro for binding affinity against Alpha-2B adrenergic receptor from cloned rat RNG receptor transfected into Chinese hamster ovary (CHO) cells | B | 8.08 | pKi | 8.3 | nM | Ki | J Med Chem (1996) 39: 3533-3538 [PMID:8784451] |
| ChEMBL | Binding affinity for rat Alpha-2B adrenergic receptor | B | 8.08 | pKi | 8.3 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Binding affinity towards alpha-2C adrenergic receptor | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2000) 43: 765-768 [PMID:10715142] |
| ChEMBL | Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscine | B | 7.25 | pKi | 56.23 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| ChEMBL | Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (1996) 39: 3533-3538 [PMID:8784451] |
| ChEMBL | Binding affinity for human Alpha-2C adrenergic receptor | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Biochim Biophys Acta (1998) 1448: 135-46 [PMID:9824686]; Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]; Eur J Pharmacol (1998) 355: 275-9 [PMID:9760042]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counter | B | 8.03 | pKi | 9.33 | nM | Ki | Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139] |
| GtoPdb | inhibition of cAMP production | - | 7.7 | pIC50 | - | - | - |
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]; Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| GtoPdb | 4.64 =value for β-arrestin recruitment and internalization | - | 6.74 | pEC50 | - | - | - | Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| ChEMBL | Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry | F | 7.24 | pEC50 | 57.54 | nM | EC50 | J Med Chem (2010) 53: 7825-7835 [PMID:20925410] |
| ChEMBL | Agonist activity at human recombinant alpha-2C receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay | F | 7.25 | pEC50 | 56 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| ChEMBL | Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate | F | 7.26 | pEC50 | 54.95 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 2317-2322 |
| GtoPdb | ERK1/2 phosphorylation | - | 7.8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73] | ||||||||
| ChEMBL | The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria | B | 4.2 | pKd | 63095.73 | nM | Kd | J Med Chem (1991) 34: 3197-3204 [PMID:1956038] |
| ChEMBL | The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria | B | 4.4 | pKd | 39810.72 | nM | Kd | J Med Chem (1991) 34: 3197-3204 [PMID:1956038] |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.48 | pIC50 | 33300 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 7.26 | pKi | 55 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 7.26 | pKi | 54.95 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Binding affinity for imidazoline receptor I-1 | B | 8 | pKi | <10 | nM | Ki | J Med Chem (1995) 38: 3681-3716 [PMID:7562902] |
| ChEMBL | Displacement of [3H]-clonidine from bovine imidazoline receptor I-1 | B | 8.05 | pKi | 8.9 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017] | ||||||||
| ChEMBL | Displacement of [3H]paraiodoclonidine from imidazoline I1 receptor in rat PC12 cells after 30 mins by gamma counter | B | 6.55 | pKi | 281.84 | nM | Ki | Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139] |
| ChEMBL | Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method | B | 6.9 | pKi | 125.89 | nM | Ki | Bioorg Med Chem (2016) 24: 3174-3183 [PMID:27265687] |
| ChEMBL | Binding affinity to I1 imidazoline binding site in Rattus norvegicus (rat) PC12 cells | B | 6.95 | pKi | 112.2 | nM | Ki | Med Chem Res (2004) 13: 170-189 |
| ChEMBL | Displacement of [125I] PIC from I1 imidazoline receptor in rat PC12 cells after 45 mins by gamma counting | B | 7.85 | pKi | 14.1 | nM | Ki | J Med Chem (2015) 58: 878-887 [PMID:25521963] |
| ChEMBL | Displacement of [3H]clonidine from imidazoline I1 receptor in Sprague-Dawley rat kidney by liquid scintillation counting | B | 6.44 | pIC50 | 366.2 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1009-1011 [PMID:19101144] |
| ChEMBL | Inhibition of Sprague-Dawley rat imidazoline I1 receptor | B | 6.44 | pIC50 | 366.2 | nM | IC50 | Bioorg Med Chem (2011) 19: 156-167 [PMID:21159515] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation | F | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (1996) 39: 570-581 [PMID:8558529] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins | B | 5.49 | pKi | 3235.94 | nM | Ki | ACS Med Chem Lett (2012) 3: 535-539 [PMID:24900506] |
| 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 | 5.51 | pKi | 3066 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 5.27 | pIC50 | 5365 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells | F | 6.26 | pKi | 550 | nM | Ki | J Pharmacol Exp Ther (1998) 286: 354-361 [PMID:9655880] |
| GtoPdb | - | - | 6.26 | pKi | 550 | nM | Ki | J Pharmacol Exp Ther (1998) 286: 354-61 [PMID:9655880] |
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.65 | pIC50 | 22600 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
| ChEMBL | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | B | 4.72 | pIC50 | 18980 | nM | IC50 | J Med Chem (2017) 60: 2685-2696 [PMID:28230985] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake in OCT1-expressing HEK293 cells | F | 5.85 | pKi | 1400 | nM | Ki | Naunyn Schmiedebergs Arch Pharmacol (1996) 354: 320-326 [PMID:8878062] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.2 uM) in OCT3-expressing HEK293 cells | F | 4.1 | pIC50 | 79300 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 40-49 [PMID:11191835] |
| HCN1 in Mouse [GtoPdb: 400] [UniProtKB: O88704] | ||||||||
| GtoPdb | - | - | 4.4 | pIC50 | - | - | - | Circulation (2007) 115: 872-80 [PMID:17261653] |
| HCN2 in Mouse [GtoPdb: 401] [UniProtKB: O88703] | ||||||||
| GtoPdb | - | - | 5.09 | pIC50 | 8090 | nM | IC50 | Circulation (2007) 115: 872-80 [PMID:17261653] |
| HCN4 in Mouse [GtoPdb: 403] [UniProtKB: O70507] | ||||||||
| GtoPdb | - | - | 5.01 | pIC50 | 9680 | nM | IC50 | Circulation (2007) 115: 872-80 [PMID:17261653] |
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]
