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ChEMBL ligand: CHEMBL420060 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones. | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
ChEMBL | Binding affinity was tested on human Alpha-1A adrenergic receptor | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
GtoPdb | - | - | 9.2 | pKi | - | - | - |
FEBS Lett (1998) 422: 279-83 [PMID:9490024]; Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; J Pharmacol Exp Ther (1997) 281: 1272-83 [PMID:9190863]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]; J Pharmacol Exp Ther (1996) 278: 136-44 [PMID:8764344]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
ChEMBL | The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones. | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
ChEMBL | In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824] | ||||||||
ChEMBL | Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay | F | 8.4 | pKd | 3.98 | nM | Kd | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
GtoPdb | - | - | 9 | pKi | - | - | - | J Biol Chem (2001) 276: 25366-71 [PMID:11331292] |
ChEMBL | Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Binding affinity against Alpha-1B adrenergic receptor from hamster clones. | B | 6.27 | pKi | 535 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
ChEMBL | The compound was tested for binding affinity against Alpha-1B adrenergic receptor, from human clones. | B | 7.04 | pKi | 92 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
ChEMBL | Binding affinity was tested on human Alpha-1B adrenergic receptor | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
GtoPdb | - | - | 7.7 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | Binding affinity against Alpha-1D adrenergic receptor, from human clones. | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
GtoPdb | - | - | 8 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
ChEMBL | Binding affinity against Alpha-1D adrenergic receptor, from rat clones. | B | 6.73 | pKi | 186 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
ChEMBL | Overall binding displacement in tissues containing only the Alpha-1B adrenergic receptor (rat spleen, rat liver) | B | 7.02 | pKi | 96 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones. | B | 6.21 | pKi | 612 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | Binding affinity against Alpha-2B adrenergic receptor from human clones. | B | 6.39 | pKi | 406 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | Binding affinity against Alpha-2C adrenergic receptor from human clones. | B | 6.88 | pKi | 131 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
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]