[3H]brimonidine (UK14304) [Ligand Id: 5386] 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] | ||||||||
| GtoPdb | - | - | 9.1 | pKd | - | - | - | Mol Pharmacol (1985) 28: 475-86 [PMID:2865672] |
| 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] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.53 | pIC50 | 298 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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) |
| 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 |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 5.98 | pIC50 | 1047 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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 |
| 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] |
| 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) |
| 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 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]
