rauwolscine [Ligand Id: 136] 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: CHEMBL10347 (Rauwolscine)
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A2b receptorpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 Bovine01234567Highcharts.com
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1b adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1d adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • Alpha-2a adrenergic receptor in Bovine [ChEMBL: CHEMBL4744] [UniProtKB: Q28838]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 Bovine0246810Highcharts.com
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2b adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2c adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 1a (5-HT1a) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuSerotonin transporterpKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
Created with Highcharts 10.3.3ValuesChart context menuVoltage-gated L-type calcium channel alpha-1C subunitpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
Created with Highcharts 10.3.3ValuesChart context menu5-HT1B receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
Created with Highcharts 10.3.3ValuesChart context menu5-HT1D receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
Created with Highcharts 10.3.3ValuesChart context menu5-ht1e receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
Created with Highcharts 10.3.3ValuesChart context menu5-HT2B receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
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 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]