brimonidine (UK14304) [Ligand Id: 520] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL844 (AGN-190342 FREE BASE, Brimonidine, NSC-318825, UK-14304, UK-1430418 FREE BASE) |
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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 for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin | B | 5.55 | pKi | 2818.38 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| 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 | 5.95 | pEC50 | 1132 | 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 | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.59 | pKi | 2568 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.2 | pIC50 | 6344 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity for human Alpha-1B adrenergic receptor from cultured LM(tk-) cells using [3H]prazosin | B | 5.27 | pKi | 5370.32 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| 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 | 6.03 | pEC50 | 943 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Binding affinity for human Alpha-1D adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin | B | 6.03 | pKi | 933.25 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.07 | pKi | 846 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.76 | pIC50 | 1720 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.95 | pKi | 112 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine | B | 8.17 | pKi | 6.76 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| ChEMBL | Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (1997) 40: 18-23 [PMID:9016324] |
| GtoPdb | - | - | 8.7 | 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]; Trends Pharmacol Sci (1997) 18: 211-9 [PMID:9227000]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.53 | pIC50 | 298 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 8.9 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells | F | 8.39 | pEC50 | 4.1 | nM | EC50 | J Med Chem (1997) 40: 18-23 [PMID:9016324] |
| 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 | 9.07 | pEC50 | 0.86 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| GtoPdb | increased ERK1/2 phosphorylation | - | 9.1 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate | F | 9.21 | pEC50 | 0.62 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| 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 | 6.32 | pKi | 478 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity for human Alpha-2B adrenergic receptor from cultured Y-1 cells using [3H]rauwolscine | B | 7.46 | pKi | 34.67 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| GtoPdb | - | - | 8.3 | 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 | 5.98 | pIC50 | 1047 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 8.4 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Alpha-2B adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis | F | 6.55 | pEC50 | 281.84 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| GtoPdb | cAMP generation | - | 7.2 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.8 | 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 | Displacement of rauwolscine from rat Alpha-2B adrenergic receptor expressed in CHO cells | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (1997) 40: 18-23 [PMID:9016324] |
| ChEMBL | Effective Concentration at Alpha-2B adrenergic receptor from CHO-RNG cells | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (1997) 40: 18-23 [PMID:9016324] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin | B | 7.08 | pKi | 83.18 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| ChEMBL | Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells | B | 7.36 | pKi | 44 | nM | Ki | J Med Chem (1997) 40: 18-23 [PMID:9016324] |
| GtoPdb | - | - | 7.6 | 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]; Trends Pharmacol Sci (1997) 18: 211-9 [PMID:9227000]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of cAMP production | - | 8.5 | pIC50 | - | - | - |
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]; Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| GtoPdb | 5.88 = value for β-arrestin recruitment and internalization | - | 6.88 | pEC50 | - | - | - | Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| ChEMBL | Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis | F | 8.02 | pEC50 | 9.55 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2255-2258 |
| 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 | 8.1 | pEC50 | 8 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| GtoPdb | ERK1/2 phosphorylation | - | 8.2 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells | F | 8.47 | pEC50 | 3.4 | nM | EC50 | J Med Chem (1997) 40: 18-23 [PMID:9016324] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| 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 | 5.84 | pKi | 1458 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 5.59 | pIC50 | 2551 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
