BRL 37344 [Ligand Id: 567] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL284782 (BRL-37344)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
1 CHEMBL284782_lig_chart_1 Beta-1 adrenergic receptor HumanRat
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Dog [ChEMBL: CHEMBL2289] [UniProtKB: P54833]
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Rat [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
2 CHEMBL284782_lig_chart_2 Beta-2 adrenergic receptor HumanDogRat
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
  • β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962]
  • β3-adrenoceptor/Beta-3 adrenergic receptor in Rat [ChEMBL: CHEMBL4031] [GtoPdb: 30] [UniProtKB: P26255]
3 CHEMBL284782_lig_chart_3 Beta-3 adrenergic receptor HumanMouseRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand. B 4.95 pKi 11300 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2253-2258
ChEMBL Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cells B 5.95 pKi 1130 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 1583-1588
ChEMBL Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 3087-3092 [PMID:9873681]
ChEMBL Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR F 5.77 pEC50 1700 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1301-1305 [PMID:12657269]
ChEMBL Agonist activity at Homo sapiens (human) beta1 adrenoreceptor B 5.77 pEC50 1700 nM EC50 Med Chem Res (2010) 19: 1121-1140 [PMID:21170122]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Compound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol B 5.48 pIC50 3300 nM IC50 J. Med. Chem. (1992) 35: 3081-3084 [PMID:1354264]
ChEMBL In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle F 6.72 pIC50 190 nM IC50 J. Med. Chem. (1992) 35: 3081-3084 [PMID:1354264]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP B 5.55 pKi 2850 nM Ki Bioorg. Med. Chem. (2007) 15: 2533-2543 [PMID:17303428]
ChEMBL Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells B 6.2 pKi 630 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 1583-1588
ChEMBL Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand. B 6.2 pKi 630 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2253-2258
ChEMBL Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol B 5.52 pIC50 3000 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 3087-3092 [PMID:9873681]
ChEMBL Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR F 6.54 pEC50 290 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1301-1305 [PMID:12657269]
ChEMBL Agonist activity at Homo sapiens (human) beta2 adrenoreceptor F 6.54 pEC50 290 nM EC50 Med Chem Res (2010) 19: 1121-1140 [PMID:21170122]
Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833]
ChEMBL Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus F 8.04 pIC50 9.12 nM IC50 J. Med. Chem. (2003) 46: 105-112 [PMID:12502364]
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
ChEMBL Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM) B 5.89 pIC50 1300 nM IC50 J. Med. Chem. (1992) 35: 3081-3084 [PMID:1354264]
ChEMBL Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction F 8.04 pIC50 9.12 nM IC50 J. Med. Chem. (2001) 44: 1436-1445 [PMID:11311067]
ChEMBL Inhibition of spontaneous contractions in isolated rat uterus F 8.04 pIC50 9.1 nM IC50 J. Med. Chem. (2003) 46: 105-112 [PMID:12502364]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells B 6.02 pKi 960 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 1583-1588
ChEMBL Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand. B 6.02 pKi 960 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2253-2258
ChEMBL Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol B 6.18 pKi 660 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 3035-3039 [PMID:11714605]
GtoPdb - - 7 pKi 100 nM Ki Eur. J. Pharmacol. (1995) 291: 359-66 [PMID:8719421];
Mol. Pharmacol. (1993) 44: 1094-104 [PMID:7903415];
J. Pharmacol. Exp. Ther. (1994) 269: 1000-6 [PMID:7912272];
Naunyn Schmiedebergs Arch. Pharmacol. (2004) 369: 151-9 [PMID:14730417]
ChEMBL Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes F 6.17 pEC50 680 nM EC50 Bioorg. Med. Chem. Lett. (1997) 7: 1583-1588
ChEMBL Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane. F 6.17 pEC50 680 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 2253-2258
ChEMBL Compound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonist F 6.35 pEC50 450 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 3087-3092 [PMID:9873681]
ChEMBL Agonism against Beta-3 adrenergic receptor F 6.35 pEC50 450 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 3087-3092 [PMID:9873681]
ChEMBL Agonist activity at Homo sapiens (human) beta3 adrenoreceptor B 7.68 pEC50 21 nM EC50 Med Chem Res (2010) 19: 1121-1140 [PMID:21170122]
ChEMBL Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR F 7.68 pEC50 21 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1301-1305 [PMID:12657269]
ChEMBL Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay F 8.23 pEC50 5.9 nM EC50 Bioorg. Med. Chem. (2008) 16: 2473-2488 [PMID:18083578]
ChEMBL Concentration required to effect a 50% relaxation of ferret detrusor basal tone F 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (2003) 46: 105-112 [PMID:12502364]
ChEMBL Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone F 8.66 pEC50 2.19 nM EC50 J. Med. Chem. (2003) 46: 105-112 [PMID:12502364]
ChEMBL Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method F 8.96 pEC50 1.1 nM EC50 Bioorg. Med. Chem. (2008) 16: 2473-2488 [PMID:18083578]
ChEMBL Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR F 10.02 pEC50 0.1 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1301-1305 [PMID:12657269]
β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962]
GtoPdb - - 6.5 pKi - - - Eur. J. Pharmacol. (1995) 291: 359-66 [PMID:8719421]
β3-adrenoceptor/Beta-3 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4031] [GtoPdb: 30] [UniProtKB: P26255]
GtoPdb - - 6.5 pKi - - - Eur. J. Pharmacol. (1995) 291: 359-66 [PMID:8719421]
ChEMBL In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes. F 8.08 pEC50 8.4 nM EC50 J. Med. Chem. (1992) 35: 3081-3084 [PMID:1354264]
ChEMBL Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor F 8.66 pEC50 2.19 nM EC50 J. Med. Chem. (2001) 44: 1436-1445 [PMID:11311067]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]