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 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]
