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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
