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 |
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]; J Neurochem (1996) 67: 2096-103 [PMID:8863519]; Eur J Pharmacol (1999) 380: 171-81 [PMID:10513577]; Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052]; Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979] |
| 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 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 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 | Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant | B | 9.3 | pKi | 0.5 | nM | Ki | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
| 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 | Binding affinity to 5-HT1DR (unknown origin) assessed as inhibition constant | B | 9.3 | pKi | 0.5 | nM | Ki | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
| 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 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]
