BRL 37344 [Ligand Id: 567] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL284782 (BRL-37344) |
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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 |
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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] |
| GtoPdb | - | - | 6.5 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 |
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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] |
| GtoPdb | - | - | 6.9 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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] |
| GtoPdb | - | - | 7.5 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 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]
