yohimbine [Ligand Id: 102] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL15245 (Yohimbine, Yohimbinum)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Mouse [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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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]
  • α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • 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]
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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 Pig [ChEMBL: CHEMBL2350] [UniProtKB: P18871]
  • 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]
  • α2B-adrenoceptor/Alpha-2B adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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  • α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/D(3) dopamine receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • DNA topoisomerase I/DNA topoisomerase 1 in Human [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
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  • M-phase inducer phosphatase 1 in Human [ChEMBL: CHEMBL3775] [UniProtKB: P30304]
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  • NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
  • 5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
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  • 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in CHO cells B 7.3 pKi 50.12 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
GtoPdb - - 7.3 pKi - - - Synapse (2000) 35: 79-95 [PMID:10611634]
ChEMBL Antagonist activity at 5-HT1A receptor (unknown origin) expressed in HEK cells coexpressing Gqi5 assessed as inhibition of serotonin induced calcium mobilization preincubated for 15 mins followed by serotonin addition at EC80 and measured for 180 secs by FLIPR assay F 5 pIC50 9929 nM IC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 7.14 pKi 72 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.9 pIC50 126 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Displacement of [3H]GR125,743 from human 5-HT1B receptor expressed in CHO cells B 6.8 pKi 158.49 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
GtoPdb - - 7.6 pKi - - - Synapse (2000) 35: 79-95 [PMID:10611634];
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]
5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
GtoPdb - - 8.3 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407]
5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Displacement of [3H]GR125,743 from human 5-HT1D receptor expressed in CHO cells B 7.6 pKi 25.12 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
GtoPdb - - 7.7 pKi - - - Synapse (2000) 35: 79-95 [PMID:10611634];
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979];
Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity for 5-HT 2A in rat stomach fundus B 5.79 pKi 1621.81 nM Ki J Med Chem (1996) 39: 2773-2780 [PMID:8709108]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.33 pKi 47 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]-5HT from human 5-HT2B receptor expressed in african green monkey COS7 cells assessed as inhibition constant B 7.37 pKi 43 nM Ki J Med Chem (2023) 66: 11027-11039 [PMID:37584406]
GtoPdb - - 7.9 pKi - - - Mol Pharmacol (1994) 46: 227-34 [PMID:8078486];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568];
Br J Pharmacol (1999) 127: 1075-82 [PMID:10455251]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.13 pIC50 74 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 7.3 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
ChEMBL Binding affinity analysed towards 5-HT 2C in rat stomach fundus B 5 pKi >10000 nM Ki J Med Chem (1996) 39: 2773-2780 [PMID:8709108]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.11 pKi 784 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.77 pIC50 1689 nM IC50 DrugMatrix in vitro pharmacology data
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor B 6.4 pKd 398.11 nM Kd J Med Chem (1984) 27: 495-503 [PMID:6142954]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells B 5.98 pKi 1057 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [3H]prazosin from human ADRA1A expressed in CHO cells B 6.7 pKi 199.53 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Antagonist activity at human ADRA1A adrenergic receptor overexpressed in rat Chem-1 cells assessed as inhibition of epinephrine induced calcium flux preincubated for 30 mins followed by incubation under dark condition for 15 mins and further incubated with epinephrine for 15 mins by Fluo-8-AM dye based assay F 5.85 pIC50 1403 nM IC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
Alpha-1A adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand B 6.66 pKi 220 nM Ki J Med Chem (1983) 26: 1696-1701 [PMID:6139479]
ChEMBL Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex B 6.66 pKi 220 nM Ki J Med Chem (1985) 28: 1756-1759 [PMID:2999400]
ChEMBL Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor B 6.7 pKi 200 nM Ki J Med Chem (1984) 27: 1182-1185 [PMID:6088770]
ChEMBL Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal B 8.44 pKi 3.6 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 6.3 pKi 500 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.91 pIC50 1235 nM IC50 DrugMatrix in vitro pharmacology data
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 6.02 pKi 966 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [3H]prazosin from human ADRA1B expressed in CHO cells B 6.8 pKi 158.49 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 8.14 pKi 7.2 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 8.96 pKi 1.1 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.18 pKi 658 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.93 pIC50 1188 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.3 pKi 498 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1D adrenergic receptor expressed in CHO cells B 6.54 pKi 289 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [3H]prazosin from human ADRA1D expressed in CHO cells B 6.8 pKi 158.49 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 8.8 pKi 1.6 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.99 pIC50 1013 nM IC50 DrugMatrix in vitro pharmacology data
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 7.28 pKi 52 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 Binding affinity to human ADRA2A adrenergic receptor overexpressed in rat Chem-1 cells assessed as dissociation constant by SPR analysis B 8.09 pKd 8.1 nM Kd J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Displacement of [3H]-yohimbine from human ADRA2A adrenergic receptor overexpressed in rat Chem-1 cells assessed as dissociation constant measured after 30 mins by microbeta2 liquid scintillation counting analysis B 8.32 pKd 4.8 nM Kd J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor B 8.12 pKi 7.5 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [3H]RX821,002 from human ADRA2A expressed in platelets B 8.2 pKi 6.31 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Displacement of [3H]RX821,002 from human ADRA2A expressed in CHO cells B 8.2 pKi 6.31 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins B 8.5 pKi 3.13 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor B 8.51 pKi 3.1 nM Ki J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins B 8.51 pKi 3.1 nM Ki Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2A receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control B 8.52 pKi 3 nM Ki J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2A receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control B 8.58 pKi 2.63 nM Ki J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.64 pKi 2.31 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL In vitro binding affinity towards alpha-2a adrenergic receptor B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2005) 15: 2758-2760 [PMID:15911252]
GtoPdb - - 9.2 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand B 9.38 pKi 0.42 nM Ki Bioorg Med Chem Lett (2000) 10: 627-630 [PMID:10762040]
ChEMBL Antagonist activity at human ADRA2A adrenergic receptor overexpressed in rat Chem-1 cells assessed as inhibition of epinephrine induced calcium flux preincubated for 30 mins followed by incubation under dark condition for 15 mins and further incubated with epinephrine for 15 mins by Fluo-8-AM dye based assay F 7.82 pIC50 15 nM IC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Antagonist activity at ADRA2A (unknown origin) expressed in CHO cells coexpressing Gqi5 assessed as inhibition of brimonidine induced calcium mobilization preincubated for 15 mins followed by brimonidine addition at EC80 and measured for 180 secs by FLIPR assay F 8.03 pIC50 9.3 nM IC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins B 8.08 pIC50 8.4 nM IC50 Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.21 pIC50 6.15 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]-yohimbine from human ADRA2A adrenergic receptor overexpressed in rat Chem-1 cells measured after 30 mins by microbeta2 liquid scintillation counting analysis B 7.82 pEC50 15 nM EC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells B 8.07 pEC50 8.5 nM EC50 J Nat Prod (2006) 69: 432-435 [PMID:16562853]
Alpha-2A adrenergic receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2350] [UniProtKB: P18871]
ChEMBL Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone B 8.36 pKi 4.4 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
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 7.31 pKi 49 nM Ki J Med Chem (1983) 26: 1696-1701 [PMID:6139479]
ChEMBL Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex B 7.31 pKi 49 nM Ki J Med Chem (1985) 28: 1756-1759 [PMID:2999400]
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2B receptor (unknown origin) B 7.54 pKi 28.84 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2B receptor expressed in human CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control B 8.03 pKi 9.33 nM Ki J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2B receptor expressed in human CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control B 8.05 pKi 9 nM Ki J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 8.1 pKi 7.95 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL In vitro binding affinity towards alpha-2b adrenergic receptor B 8.15 pKi 7.1 nM Ki Bioorg Med Chem Lett (2005) 15: 2758-2760 [PMID:15911252]
ChEMBL Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2B adrenergic receptor B 8.34 pKi 4.6 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2B receptor (unknown origin) B 8.49 pKi 3.2 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Binding affinity against human alpha 2b-adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand B 8.7 pKi 2.01 nM Ki Bioorg Med Chem Lett (2000) 10: 627-630 [PMID:10762040]
ChEMBL Displacement of [3H]RX821,002 from human ADRA2B expressed in CHO cells B 8.7 pKi 2 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes incubated for 60 mins B 8.94 pKi 1.16 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL Antagonist activity at ADRA2B (unknown origin) expressed in CHO cells coexpressing Gqi5 assessed as inhibition of brimonidine induced calcium mobilization preincubated for 15 mins followed by brimonidine addition at EC80 and measured for 180 secs by FLIPR assay F 7.06 pIC50 86.6 nM IC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.77 pIC50 17 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Inhibition of [3H]- Yohimbine binding against rat kidney cortex Alpha-2B adrenergic receptor B 8.7 pKi 2 nM Ki J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 8.29 pKi 5.16 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor B 8.64 pKi 2.3 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2C receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control B 8.7 pKi 2 nM Ki J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2C receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control B 8.81 pKi 1.55 nM Ki J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine B 9.06 pKi 0.88 nM Ki Bioorg Med Chem Lett (2005) 15: 2758-2760 [PMID:15911252]
ChEMBL Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 mins B 9.1 pKi 0.8 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
GtoPdb - - 9.5 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL Displacement of [3H]RX821,002 from human ADRA2C expressed in CHO cells B 9.6 pKi 0.25 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 7.44 pIC50 36 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonist activity at ADRA2C (unknown origin) expressed in CHO cells coexpressing Gqi5 assessed as inhibition of brimonidine induced calcium mobilization preincubated for 15 mins followed by brimonidine addition at EC80 and measured for 180 secs by FLIPR assay F 8.11 pIC50 7.7 nM IC50 J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
GtoPdb - - 8.2 pIC50 - - - Brain Res Bull (2014) 107: 89-101 [PMID:25080296]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Binding affinity to human beta 2 adrenergic receptor assessed as inhibition constant B 10.4 pKi 0.04 nM Ki RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.69 pIC50 2031.7 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.16 pKi 687 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Spiperone from human D2 receptor expressed in CHO cells B 6.4 pKi 398.11 nM Ki J Med Chem (2024) 67: 10135-10151 [PMID:38857067]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.69 pIC50 2060 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro inhibition of specific binding of [3H]-YM 09151-2 to Dopamine receptor D2 site in rat striatal tissue. B 5.95 pIC50 1125 nM IC50 J Med Chem (2000) 43: 3653-3664 [PMID:11020279]
D3 receptor/D(3) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 5.61 pKi 2430 nM Ki J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
DNA topoisomerase I/DNA topoisomerase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
ChEMBL Inhibition of human recombinant DNA topoisomerase1 B 4.52 pIC50 30000 nM IC50 J Nat Prod (2005) 68: 848-852 [PMID:15974606]
M-phase inducer phosphatase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3775] [UniProtKB: P30304]
ChEMBL Inhibition of His-tagged Cdc25A expressed in the Escherichia coli BL21(DE3) using p-nitrophenyl phosphate as substrate for 80 mins by spectrophotometry B 4.65 pIC50 22300 nM IC50 J Med Chem (2012) 55: 5989-6001 [PMID:22537178]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum incubated for 72 hrs by SYBR green I-based assay F 4.3 pEC50 >50000 nM EC50 Eur J Med Chem (2021) 221: 113536-113536 [PMID:34058709]
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation F 4.7 pIC50 >20000 nM IC50 J Med Chem (1996) 39: 570-581 [PMID:8558529]
Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C 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 7.35 pKi 45 nM Ki J Med Chem (1995) 38: 3681-3716 [PMID:7562902]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 5.9 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 7 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
GtoPdb - - 6.2 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 2184-8 [PMID:8384716]
5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
GtoPdb - - 5.3 pKi - - - FEBS Lett (1994) 355: 242-6 [PMID:7988681]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 6 pKi - - - Mol Pharmacol (1993) 43: 313-9 [PMID:8450829];
FEBS Lett (1995) 377: 451-6 [PMID:8549774]
5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 5.6 pKi - - - J Biol Chem (1993) 268: 23422-6 [PMID:8226867]

ChEMBL data shown on this page come from version 36:

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]