[3H]brimonidine [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)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • Alpha-1B adrenergic receptor in Cricetulus griseus [ChEMBL: CHEMBL3988626] [UniProtKB: G3HDX1]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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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]
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]