sumatriptan [Ligand Id: 54] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL128 (Dfn-11, Dfn-11 (sumatriptan injection), Imitrex, N02CC01, Sumatriptan, Tosymra) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine 1D receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638336] [UniProtKB: Q8MI13] | ||||||||
| ChEMBL | Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12). | B | 7.23 | pIC50 | 59 | nM | IC50 | US-8586620-B2. Substituted indole compounds having NOS inhibitory activity (2013) |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | The compound was tested for CNS binding affinity towards Dopamine receptor D2 from cloned Human membranes. | B | 6.66 | pKi | >218 | nM | Ki | J Med Chem (1998) 41: 2180-2183 [PMID:9632349] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity for rat dopamine D2 receptor expressed in CHO-K1 cells | B | 6.66 | pKi | >218 | nM | Ki | J Med Chem (1996) 39: 4717-4726 [PMID:8941384] |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.17 | pIC50 | 6700 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor in piglet hippocampus using [3H]8-OH-DPAT | B | 5.5 | pKd | 5.5 | - | pKD | J Med Chem (1993) 36: 1918-1919 [PMID:8515429] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 6.4 | pKd | 398.11 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| GtoPdb | - | - | 6 | pKi | - | - | - | Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxy tryptamine 1A (5-HT1A) receptor was determined | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 663-666 |
| ChEMBL | Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1A receptor in CHO-K1 cells | F | 6.36 | pKi | 440 | nM | Ki | J Med Chem (1996) 39: 4920-4927 [PMID:8960551] |
| ChEMBL | Binding affinity for cloned human 5-hydroxytryptamine 1A receptor | B | 6.36 | pKi | 440 | nM | Ki | J Med Chem (1995) 38: 3602-3607 [PMID:7658447] |
| ChEMBL | In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand | B | 6.39 | pKi | 407.1 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| ChEMBL | The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1A receptor from cloned Human membranes. | B | 6.47 | pKi | 341 | nM | Ki | J Med Chem (1998) 41: 2180-2183 [PMID:9632349] |
| ChEMBL | Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1A receptor expressed in CHO-K1 cells. | B | 6.47 | pKi | 341 | nM | Ki | J Med Chem (1996) 39: 4717-4726 [PMID:8941384] |
| ChEMBL | In vitro affinity at human cloned 5-hydroxytryptamine 1A receptor by [3H]8-OH-DPAT displacement. | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 1A receptor in AK cells transfected with human 5-HT1A gene labeled with [3H]-8-OH-DPAT | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (1994) 37: 2828-2830 [PMID:8071931] |
| ChEMBL | In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (1999) 42: 526-531 [PMID:9986723] |
| ChEMBL | Binding activity radioligand. | B | 6.3 | pIC50 | 501.19 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Binding activity radioligand. | B | 6.4 | pIC50 | 398.11 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Ability to bind to 5-hydroxytryptamine 1A receptor from cloned human expressed in Ha7 cells | B | 6.4 | pIC50 | 398.11 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2649-2654 |
| ChEMBL | Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells | F | 6 | pEC50 | >1000 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 663-666 |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] | ||||||||
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 1A receptor | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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 | 6.34 | pKi | 459 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.09 | pIC50 | 804 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity was measured against serotonin 5-hydroxytryptamine 1A receptor | B | 6.19 | pIC50 | 640 | nM | IC50 | J Med Chem (1994) 37: 2509-2512 [PMID:8057297] |
| ChEMBL | Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor | F | 5.89 | pEC50 | 1300 | nM | EC50 | J Med Chem (1994) 37: 2509-2512 [PMID:8057297] |
| Serotonin 1b (5-HT1b) receptor in Gorilla (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304408] [UniProtKB: Q9N2B7] | ||||||||
| ChEMBL | The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1998) 41: 2180-2183 [PMID:9632349] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor | B | 7.32 | pKi | 47.9 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1707-1709 [PMID:10937729] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 1B receptor | B | 7.44 | pKi | 36 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 903-905 [PMID:10853656] |
| ChEMBL | Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP. | F | 7.62 | pKi | 24 | nM | Ki | J Med Chem (1996) 39: 4717-4726 [PMID:8941384] |
| ChEMBL | Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells | F | 7.64 | pKi | 23.1 | nM | Ki | J Med Chem (1996) 39: 4920-4927 [PMID:8960551] |
| ChEMBL | The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta | B | 7.64 | pKi | 23.1 | nM | Ki | J Med Chem (1995) 38: 3602-3607 [PMID:7658447] |
| ChEMBL | Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells. | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (1996) 39: 4717-4726 [PMID:8941384] |
| ChEMBL | In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand | B | 7.72 | pKi | 19.1 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
| ChEMBL | In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor | B | 8.02 | pKi | 9.6 | nM | Ki | J Med Chem (1999) 42: 526-531 [PMID:9986723] |
| ChEMBL | Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting | B | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2008) 51: 3609-3616 [PMID:18507369] |
| GtoPdb | - | - | 8.1 | pKi | 7.94 | nM | Ki |
Eur J Pharmacol (1999) 380: 171-81 [PMID:10513577]; Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]; Synapse (2000) 35: 79-95 [PMID:10611634]; Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]; Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052]; J Neurochem (1996) 67: 2096-103 [PMID:8863519]; Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658] |
| ChEMBL | Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor | B | 8.11 | pKi | 7.7 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 727-729 [PMID:14741277] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor | B | 8.11 | pKi | 7.7 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3419-3421 [PMID:14505640] |
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (1994) 37: 2828-2830 [PMID:8071931] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| ChEMBL | Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement. | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1997) 40: 3497-3500 [PMID:9357514] |
| ChEMBL | Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells. | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1999) 42: 691-705 [PMID:10052976] |
| ChEMBL | Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1999) 42: 677-690 [PMID:10052975] |
| ChEMBL | Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1999) 42: 4981-5001 [PMID:10585208] |
| ChEMBL | Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2001) 44: 681-693 [PMID:11262079] |
| ChEMBL | Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells | F | 7.11 | pEC50 | 77 | nM | EC50 | J Med Chem (1996) 39: 4920-4927 [PMID:8960551] |
| ChEMBL | Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines | F | 7.42 | pEC50 | 38.3 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT | B | 7.64 | pKi | 23 | nM | Ki | J Med Chem (1994) 37: 2828-2830 [PMID:8071931] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) | B | 8.09 | pKi | 8.19 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12). | B | 6.96 | pIC50 | 110 | nM | IC50 | US-8586620-B2. Substituted indole compounds having NOS inhibitory activity (2013) |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) | B | 7.74 | pIC50 | 18 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor alpha measured as the reduction of forskolin-stimulated cAMP. | F | 7.52 | pKi | 30 | nM | Ki | J Med Chem (1996) 39: 4717-4726 [PMID:8941384] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined | B | 7.64 | pKi | 23.1 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 663-666 |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 1D receptor | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 903-905 [PMID:10853656] |
| ChEMBL | In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1D receptor using [3H]5-CT radioligand | B | 8.07 | pKi | 8.6 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor alpha was determined | B | 8.07 | pKi | 8.5 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 663-666 |
| ChEMBL | Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1995) 38: 3602-3607 [PMID:7658447] |
| ChEMBL | Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1D receptor in CHO-K1 cells | F | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1996) 39: 4920-4927 [PMID:8960551] |
| ChEMBL | Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells. | B | 8.24 | pKi | 5.7 | nM | Ki | J Med Chem (1996) 39: 4717-4726 [PMID:8941384] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 1D receptor | B | 8.26 | pKi | 5.5 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1707-1709 [PMID:10937729] |
| ChEMBL | In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (1999) 42: 526-531 [PMID:9986723] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3419-3421 [PMID:14505640] |
| ChEMBL | Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1D receptor | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 727-729 [PMID:14741277] |
| ChEMBL | The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1D receptor from cloned gorilla membranes expressed in cultured HEK 293 cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1998) 41: 2180-2183 [PMID:9632349] |
| GtoPdb | - | - | 8.7 | pKi | 1.99 | nM | Ki |
Synapse (2000) 35: 79-95 [PMID:10611634]; Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]; 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] |
| ChEMBL | Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2008) 51: 3609-3616 [PMID:18507369] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 1D receptor | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| ChEMBL | Ability to bind to 5-hydroxytryptamine 1D receptor of calf substantia nigra | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2649-2654 |
| ChEMBL | Binding activity radioligand. | B | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1D receptor stably expressed in CHO cells. | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (1999) 42: 4981-5001 [PMID:10585208] |
| ChEMBL | Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (1999) 42: 677-690 [PMID:10052975] |
| ChEMBL | Displacement of [3H]5-HT binding from human 5-hydroxytryptamine 1D receptor expressed in CHO cells | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (1999) 42: 691-705 [PMID:10052976] |
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| ChEMBL | Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement. | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1997) 40: 3497-3500 [PMID:9357514] |
| ChEMBL | Binding affinity in CHO-K1 cells transfected with human 5-hydroxytryptamine 1D receptor | B | 8.53 | pIC50 | 2.95 | nM | IC50 | J Med Chem (2001) 44: 681-693 [PMID:11262079] |
| ChEMBL | Compound was tested for 5-hydroxytryptamine 1D like receptor-mediated vascular effect in rabbit saphenous vein (RSV) | B | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (1998) 41: 2243-2251 [PMID:9632357] |
| ChEMBL | Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 30-70 | F | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 663-666 |
| ChEMBL | Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor. | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| ChEMBL | Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor. | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (1997) 40: 3497-3500 [PMID:9357514] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor | F | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (1999) 42: 677-690 [PMID:10052975] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor | F | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (1999) 42: 691-705 [PMID:10052976] |
| ChEMBL | Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (1999) 42: 4981-5001 [PMID:10585208] |
| ChEMBL | Ability to inhibit forskolin-stimulated adenylate cyclase activity in Chinese hamster ovary (CHO) stable cell lines expressing human 5-hydroxytryptamine 1D receptor | F | 8.28 | pEC50 | 5.3 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 4409-4413 [PMID:14643336] |
| ChEMBL | Ability to inhibit forskolin-stimulated adenylate cyclase in a cell line expressing human 5-hydroxytryptamine 1D receptor | F | 8.37 | pEC50 | 4.3 | nM | EC50 | J Med Chem (1999) 42: 526-531 [PMID:9986723] |
| Serotonin 1d (5-HT1d) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105] [UniProtKB: P79400] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1D receptor in piglet caudate using [3H]5-HT | B | 7.6 | pKd | 7.6 | - | pKD | J Med Chem (1993) 36: 1918-1919 [PMID:8515429] |
| ChEMBL | Binding activity radioligand. | B | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Displacement of radioligand [3H]5-HT binding to 5-hydroxytryptamine 1D receptor in pig caudate membrane | B | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (1993) 36: 1529-1538 [PMID:8496922] |
| ChEMBL | Displacement of [3H]5-HT binding to 5-hydroxytryptamine 1D receptor from pig caudate membrane | B | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (1994) 37: 3023-3032 [PMID:7932524] |
| ChEMBL | Compound was tested for the displacement of [3H]-5-HT to 5-hydroxytryptamine 1D receptor recognition sites in pig caudate membranes | B | 7.7 | pIC50 | 19.95 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 993-997 |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565] | ||||||||
| ChEMBL | Binding affinity was measured against serotonin 5-hydroxytryptamine 1D receptor | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (1994) 37: 2509-2512 [PMID:8057297] |
| ChEMBL | Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor | F | 7.01 | pEC50 | 97 | nM | EC50 | J Med Chem (1994) 37: 2509-2512 [PMID:8057297] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - |
Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]; J Neurochem (1996) 67: 2096-103 [PMID:8863519]; Proc Natl Acad Sci USA (1992) 89: 5517-21 [PMID:1608964]; Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 1E receptor | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 1F receptor was determined | B | 7.59 | pKi | 25.7 | nM | Ki | J Med Chem (2001) 44: 4031-4034 [PMID:11708905] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2005) 371: 169-77 [PMID:15900510]; Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]; Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Neuropharmacology (1997) 36: 569-76 [PMID:9225282] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 1F receptor | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| GtoPdb | - | - | 7.2 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 2184-8 [PMID:8384716] |
| ChEMBL | In vitro effective concentration for inhibition of skolin-stimulated adenylate cyclase in cell line expressing human 5-hydroxytryptamine 1F receptor | F | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2001) 44: 4031-4034 [PMID:11708905] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 2A receptor in GF6 cells transfected with human 5-HT2A gene labeled with [3H]ketanserin | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1994) 37: 2828-2830 [PMID:8071931] |
| ChEMBL | The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 2A receptor from cloned Human membranes | B | 6.42 | pKi | 376 | nM | Ki | J Med Chem (1998) 41: 2180-2183 [PMID:9632349] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 2A receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| ChEMBL | Binding activity radioligand. | B | 5.1 | pIC50 | 7943.28 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding activity radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Displacement of [3H]DOB binding to 5-hydroxytryptamine 2A receptor from rat cortex homogenate | B | 5 | pIC50 | <10000 | nM | IC50 | J Med Chem (1994) 37: 3023-3032 [PMID:7932524] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1C receptor in piglet choroid plexus using [3H]5-HT | B | 4.8 | pKd | 4.8 | - | pKD | J Med Chem (1993) 36: 1918-1919 [PMID:8515429] |
| ChEMBL | Binding activity radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Binding activity radioligand. | B | 5.1 | pIC50 | 7943.28 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 2C receptor | B | 8.14 | pIC50 | 7.3 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 2C receptor in J1 cells transfected with rat 5-HT2C gene labeled with [3H]mesulergine | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1994) 37: 2828-2830 [PMID:8071931] |
| 5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| ChEMBL | Binding activity radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 3 receptor in NG-108 cells labeled with [3H]GR-65630 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1994) 37: 2828-2830 [PMID:8071931] |
| ChEMBL | Displacement of [3H]-Q-ICS 205-930 binding to 5-hydroxytryptamine 3 receptor from rat cortex homogenate | B | 5 | pIC50 | <10000 | nM | IC50 | J Med Chem (1994) 37: 3023-3032 [PMID:7932524] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Binding activity radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Compound was evaluated for the affinity at 5-hydroxytryptamine 3 receptor | B | 8.03 | pIC50 | 9.3 | nM | IC50 | J Med Chem (1997) 40: 3501-3503 [PMID:9357515] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | - | - | - |
FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| ChEMBL | Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex | B | 6.3 | pIC50 | 501.19 | nM | IC50 | J Med Chem (1994) 37: 3023-3032 [PMID:7932524] |
| 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| GtoPdb | - | - | 4.8 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 313-9 [PMID:8450829]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - |
Br J Pharmacol (1997) 122: 126-32 [PMID:9298538]; J Biol Chem (1993) 268: 23422-6 [PMID:8226867] |
| ChEMBL | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | B | 6 | pKi | 1000 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - |
J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
| 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | J Neurochem (1996) 66: 47-56 [PMID:8522988] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | J Neurochem (1998) 71: 2169-77 [PMID:9798944] |
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]
