5-methylurapidil [Ligand Id: 489] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL420060
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • Alpha-1a adrenergic receptor in Rabbit [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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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]
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 - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
FEBS Lett (1998) 422: 279-83 [PMID:9490024];
J Pharmacol Exp Ther (1996) 278: 136-44 [PMID:8764344];
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]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]