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 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]
