rauwolscine [Ligand Id: 136] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL10347 (Rauwolscine)
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
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  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
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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]
  • Alpha-2a adrenergic receptor in Bovine [ChEMBL: CHEMBL4744] [UniProtKB: Q28838]
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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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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
ChEMBL Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus. B 7.02 pKd 95.5 nM Kd J. Med. Chem. (1983) 26: 823-831 [PMID:6133953]
ChEMBL In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine F 7.86 pKd 13.8 nM Kd J. Med. Chem. (1983) 26: 823-831 [PMID:6133953]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells B 5.36 pKi 4400 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor B 6.03 pKi 940 nM Ki J. Med. Chem. (1984) 27: 1182-1185 [PMID:6088770]
ChEMBL Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand B 6.03 pKi 940 nM Ki J. Med. Chem. (1983) 26: 1696-1701 [PMID:6139479]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1B adrenergic receptor expressed in CHO cells B 5.64 pKi 2270 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL The compound was tested for binding affinity against Alpha-1B adrenergic receptor, from human clones. B 8.34 pKi 4.6 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1D adrenergic receptor expressed in CHO cells B 5.88 pKi 1320 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
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 7.46 pKi 35 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 Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor B 8.34 pKi 4.6 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
GtoPdb - - 8.4 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470]
Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838]
ChEMBL Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand B 7.74 pKi 18 nM Ki J. Med. Chem. (1983) 26: 1696-1701 [PMID:6139479]
ChEMBL Compound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pineal B 8.47 pKi 3.4 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]
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470]
ChEMBL Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2B adrenergic receptor B 8.33 pKi 4.7 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor B 9 pKi 1 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
GtoPdb - - 9.1 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470]
ChEMBL Antagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulation F 7.8 pIC50 16 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to 5HT1A receptor B 7.4 pKd 39.81 nM Kd J. Med. Chem. (2009) 52: 6107-6125 [PMID:19754201]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of uptake of [3H]5-HT in synaptosomes from rat cortex F 5 pIC50 >10000 nM IC50 J. Med. Chem. (1997) 40: 1049-1062 [PMID:9089327]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of [3H]nitrendipine binding to membrane homogenates of rat cardiac muscle. B 7.4 pKi 40 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 7.4 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
J Neurochem (1996) 67: 2096-103 [PMID:8863519]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 7.8 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 5.5 pKi - - - J Neurochem (1996) 67: 2096-103 [PMID:8863519];
Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 8.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 7.4 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]