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ChEMBL ligand: CHEMBL39 (5-HT, 5-Hydroxytryptamine, Enteramine, Serotonin, Thrombotonin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells | B | 5.01 | pKd | 9690 | nM | Kd | J. Med. Chem. (1996) 39: 850-859 [PMID:8632409] |
GtoPdb | - | - | 5 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand | B | 6.28 | pEC50 | 523 | nM | EC50 | J. Med. Chem. (2003) 46: 3822-3839 [PMID:12930145] |
D3 receptor/Dopamine D3 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 | 5.63 | pKi | 2338 | nM | Ki | J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771] |
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
ChEMBL | Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells | B | 4 | pKi | >100000 | nM | Ki | Bioorg. Med. Chem. Lett. (1997) 7: 2409-2414 |
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells | B | 4 | pKi | >100000 | nM | Ki | Bioorg. Med. Chem. Lett. (1997) 7: 2409-2414 |
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 was determined | B | 8.5 | pKd | 8.5 | - | pKD | J. Med. Chem. (1993) 36: 1918-1919 [PMID:8515429] |
ChEMBL | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | B | 5 | pKi | 10000 | nM | Ki | J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113] |
ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting | B | 7.3 | pKi | <50 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 3345-3351 [PMID:20363635] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293-EBNA cells after 120 mins | B | 8.02 | pKi | 9.5 | nM | Ki | Eur. J. Med. Chem. (2013) 69: 920-930 [PMID:24161678] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 8.26 | pKi | 5.5 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1A human cloned receptors in HEK293 cells using [3H]8-OH-DPAT as radioligand | B | 8.4 | pKi | 3.98 | nM | Ki | J. Med. Chem. (2003) 46: 5117-5120 [PMID:14613313] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting method | B | 8.44 | pKi | 3.6 | nM | Ki | Eur J Med Chem (2019) 180: 383-397 [PMID:31325785] |
ChEMBL | In vitro inhibition of [3H]DPAT (1 nM) binding to 5-HT1A receptor from bovine hippocampus | B | 8.52 | pKi | 3 | nM | Ki | J. Med. Chem. (1989) 32: 543-547 [PMID:2918500] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from recombinant human 5HT1A receptor expressed in CHO cell membranes measured after 60 mins by microbeta scintillation counting analysis | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2019) 166: 144-158 [PMID:30703658] |
ChEMBL | In vitro inhibition of [3H]DPAT (1 nM) binding to 5-hydroxytryptamine 1A receptor from bovine hippocampus | B | 8.55 | pKi | 2.8 | nM | Ki | J. Med. Chem. (1989) 32: 543-547 [PMID:2918500] |
ChEMBL | The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1A receptor | B | 8.6 | pKi | 2.5 | nM | Ki | J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447] |
ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.61 | pKi | 2.48 | nM | Ki | Bioorg. Med. Chem. Lett. (1998) 8: 1407-1412 [PMID:9871775] |
ChEMBL | Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1A receptor in CHO-K1 cells | F | 8.61 | pKi | 2.48 | nM | Ki | J. Med. Chem. (1996) 39: 4920-4927 [PMID:8960551] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 8.68 | pKi | 2.08 | nM | Ki | Eur. J. Med. Chem. (2014) 85: 716-726 [PMID:25128671] |
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 | 8.77 | pKi | 1.7 | nM | Ki | J. Med. Chem. (1994) 37: 2828-2830 [PMID:8071931] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta scintillation counting analysis | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2018) 26: 527-535 [PMID:29269256] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2017) 60: 7483-7501 [PMID:28763213] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting method | B | 8.89 | pKi | 1.3 | nM | Ki | Eur J Med Chem (2017) 137: 108-116 [PMID:28575721] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | B | 8.9 | pKi | 1.26 | nM | Ki | J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by microbeta2 scintillation counter | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 60 mins by microbeta scintillation counting method | B | 8.96 | pKi | 1.1 | nM | Ki | MedChemComm (2017) 8: 1690-1696 [PMID:30108880] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 9.04 | pKi | 0.91 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
ChEMBL | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor (unknown origin) expressed in HEK293 cells by liquid scintillation counter | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg. Med. Chem. (2013) 21: 856-868 [PMID:23332346] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells | B | 9.21 | pKi | 0.62 | nM | Ki | Bioorg. Med. Chem. (2012) 20: 4862-4871 [PMID:22748706] |
GtoPdb | - | - | 9.7 | pKi | - | - | - |
Biochem J (1992) 285 ( Pt 3): 933-8 [PMID:1386736]; Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]; Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 682-8 [PMID:9205951]; Biosci Rep (2004) 24: 101-15 [PMID:15628665] |
ChEMBL | In vitro inhibition of [3H]5-HT (2 nM) binding to 5-hydroxytryptamine 1A receptor from bovine hippocampus | B | 8.22 | pIC50 | 6 | nM | IC50 | J. Med. Chem. (1989) 32: 543-547 [PMID:2918500] |
ChEMBL | In vitro inhibition of [3H]5-HT (2 nM) binding to 5-HT1A receptor from bovine hippocampus | B | 8.25 | pIC50 | 5.6 | nM | IC50 | J. Med. Chem. (1989) 32: 543-547 [PMID:2918500] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J. Med. Chem. (1992) 35: 4503-4505 [PMID:1447752] |
ChEMBL | In vitro inhibition of [125I]IPAPP (0.25 nM) binding to 5-HT1A receptor from bovine hippocampus | B | 8.7 | pIC50 | 2 | nM | IC50 | J. Med. Chem. (1989) 32: 543-547 [PMID:2918500] |
ChEMBL | In vitro inhibition of azido-[125I]-IPAPP (0.25 nM) binding to 5-HT1A receptor from bovine hippocampus | B | 8.7 | pIC50 | 2 | nM | IC50 | J. Med. Chem. (1989) 32: 543-547 [PMID:2918500] |
ChEMBL | In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071] |
ChEMBL | Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay | B | 5.74 | pEC50 | 1800 | nM | EC50 | J Nat Prod (2019) 82: 3302-3310 [PMID:31789520] |
ChEMBL | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | F | 6.64 | pEC50 | 229.09 |