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 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]
