(+)-cyclazosin [Ligand Id: 486] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL423294 (Cyclazosin)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
There should be some charts here, you may need to enable JavaScript!
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 Binding affinity was tested on human Alpha-1A adrenergic receptor B 7.6 pKi 25.12 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 7.9 pKi - - - J Med Chem (1996) 39: 4602-7 [PMID:8917649]
ChEMBL Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells B 7.91 pKi 12.3 nM Ki Bioorg. Med. Chem. (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method B 7.91 pKi 12.3 nM Ki Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells B 8.26 pKi 5.5 nM Ki J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay B 8.62 pKi 2.4 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat F 7.48 pKd 33.11 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction F 7.77 pKd 16.98 nM Kd Bioorg. Med. Chem. (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride F 7.77 pKd 16.98 nM Kd Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference F 8.91 pKd 1.23 nM Kd J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
ChEMBL Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity to human alpha1B adrenergic receptor B 9.16 pKi 0.69 nM Ki Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells B 9.49 pKi 0.32 nM Ki J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay B 9.51 pKi 0.31 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL Binding affinity was tested on cloned hamster Alpha-1B adrenergic receptor B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [3H]prazosin from human adrenergic alpha-1b receptor expressed in CHO cells B 9.87 pKi 0.13 nM Ki Bioorg. Med. Chem. (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL Displacement of [3H]prazosin from human alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method B 9.87 pKi 0.13 nM Ki Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
GtoPdb - - 9.9 pKi - - - J Med Chem (1996) 39: 4602-7 [PMID:8917649]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Antagonistic affinity against Alpha-1B adrenergic receptor was determined in isolated spleen tissue from rat F 9.16 pKd 0.69 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL Antagonist activity at rat Alpha-1B adrenoceptor assessed as inhibition if phenylephrine-induced contraction of spleen F 9.18 pKd 0.66 nM Kd J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity was tested on cloned rat Alpha-1D adrenergic receptor B 7.5 pKi 31.62 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [3H]prazosin from human adrenergic alpha-1d receptor expressed in CHO cells B 8.49 pKi 3.24 nM Ki Bioorg. Med. Chem. (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL Displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method B 8.49 pKi 3.24 nM Ki Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
GtoPdb - - 8.5 pKi - - - J Med Chem (1996) 39: 4602-7 [PMID:8917649]
ChEMBL Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells B 9.77 pKi 0.17 nM Ki J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Antagonist activity against adrenergic Alpha-1D receptor in rat thoracic aorta assessed as noradrenaline-induced response F 7.27 pKd 53.7 nM Kd Bioorg. Med. Chem. (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL Antagonist activity at alpha1D adrenergic receptor in Wistar rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction measured after 30 mins in presence of cocaine hydrochloride and beta-adrenoceptor blocker propranolol hydrochloride F 7.27 pKd 53.7 nM Kd Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL Antagonistic affinity against Alpha-1D adrenergic receptor was determined in isolated thoracic aorta from rat F 7.57 pKd 26.92 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL Antagonist activity at rat Alpha-1D adrenoceptor assessed as inhibition if norepenephrine-induced contraction of thoracic aorta F 9.21 pKd 0.62 nM Kd J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb - - 7.6 pKi - - - J Med Chem (1996) 39: 4602-7 [PMID:8917649]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1D adrenergic receptor from rat brain. B 9.24 pKi 0.58 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
Beta casein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2210] [UniProtKB: P02665]
ChEMBL Compound was tested for binding affinity against native Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay B 9.85 pKi 0.14 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Compound was tested for binding affinity against native Dopamine receptor D2 from rat striatum using radioligand [3H]-spiperone) B 5 pKi <10000 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL Antagonistic affinity against rat striatum Dopamine receptor D2 F 5.08 pKi 8317.64 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Antagonistic affinity against cloned human 5-hydroxytryptamine 1A receptor F 6 pKi <1000 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity against native 5-HT1A-receptors from rat hippocampus using radioligand ([3H]8-hydroxy-2-(di-n-propylamino)-tetraline) binding assay B 5.21 pKi 6165.95 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]

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]