rauwolscine [Ligand Id: 136] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL10347 (Rauwolscine) |
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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 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]
