A61603 [Ligand Id: 480] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL109783 |
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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] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; J Pharmacol Exp Ther (1995) 274: 97-103 [PMID:7616455]; Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate | F | 7.66 | pEC50 | 21.88 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor | B | 8.03 | pEC50 | 9.3 | nM | EC50 | J Med Chem (2002) 45: 4395-4397 [PMID:12238918] |
| GtoPdb | - | - | 10.3 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1995) 274: 97-103 [PMID:7616455]; Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Binding affinity towards bovine clonal Alpha-1A adrenergic receptor | B | 7.52 | pKi | 30.2 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay | B | 7.92 | pKi | 12.02 | nM | Ki | J Med Chem (2004) 47: 3220-3235 [PMID:15163201] |
| ChEMBL | Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015) | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2002) 45: 4395-4397 [PMID:12238918] |
| ChEMBL | Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands | B | 8.05 | pKi | 8.91 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens | F | 8.24 | pEC50 | 5.75 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| GtoPdb | - | - | 4 | pKi | >100000 | nM | Ki | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| GtoPdb | - | - | 6.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841] | ||||||||
| ChEMBL | In vitro binding affinity towards alpha-1B adrenergic receptor of hamster clone in radioligand binding assay | B | 5.53 | pKi | 2951.21 | nM | Ki | J Med Chem (2004) 47: 3220-3235 [PMID:15163201] |
| ChEMBL | Binding affinity towards hamster cloned Alpha-1B adrenergic receptor; value ranges from (2.0 -4.4) | B | 5.54 | pKi | 2900 | nM | Ki | J Med Chem (2002) 45: 4395-4397 [PMID:12238918] |
| ChEMBL | Binding affinity towards hamster clonal Alpha-1B adrenergic receptor | B | 5.68 | pKi | 2089.3 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | Effective concentration in vitro against rat spleen Alpha-1B adrenergic receptor indicates EC50 < 15% at a concentration of 10 uM | B | 6.49 | pEC50 | 320 | nM | EC50 | J Med Chem (2002) 45: 4395-4397 [PMID:12238918] |
| ChEMBL | In vitro agonist potency towards Alpha-1B adrenergic receptor in rat spleen | F | 6.5 | pEC50 | 316.23 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | Binding affinity towards rat cloned Alpha-1D adrenergic receptor; value ranges from (1.3 -1.6) | B | 5.82 | pKi | 1500 | nM | Ki | J Med Chem (2002) 45: 4395-4397 [PMID:12238918] |
| ChEMBL | In vitro binding affinity towards alpha-1D adrenergic receptor of rat clone in radioligand binding assay | B | 5.83 | pKi | 1479.11 | nM | Ki | J Med Chem (2004) 47: 3220-3235 [PMID:15163201] |
| ChEMBL | Binding affinity towards rat clonal Alpha-1D adrenergic receptor | B | 5.87 | pKi | 1348.96 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | Effective concentration in vitro against rat aorta Alpha-1D adrenergic receptor;* indicates EC50 < 15% at a concentration of 10 uM | B | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2002) 45: 4395-4397 [PMID:12238918] |
| ChEMBL | In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta | F | 5.59 | pEC50 | 2570.4 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay | B | 7.48 | pKi | 33.11 | nM | Ki | J Med Chem (2004) 47: 3220-3235 [PMID:15163201] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328] | ||||||||
| ChEMBL | In vitro binding affinity towards alpha-2B adrenergic receptor of rat neonatal lung in radioligand binding assay | B | 6.61 | pKi | 245.47 | nM | Ki | J Med Chem (2004) 47: 3220-3235 [PMID:15163201] |
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]
