methiothepin [Ligand Id: 89] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL93240 (Metitepine, Methiothepin)
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • G protein-coupled receptor in Human cytomegalovirus [ChEMBL: CHEMBL3559679] [UniProtKB: Q9IP65]
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  • Human herpesvirus 5 chemokine receptor in Human cytomegalovirus (strain AD169) (HHV-5) (Human herpesvirus 5) [ChEMBL: CHEMBL4259] [UniProtKB: P69332]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
  • 5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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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]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate B 8.7 pKi 2 nM Ki J. Med. Chem. (2002) 45: 344-359 [PMID:11784139]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2002) 45: 344-359 [PMID:11784139]
G protein-coupled receptor in Human cytomegalovirus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559679] [UniProtKB: Q9IP65]
ChEMBL Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay B 6.48 pEC50 331.13 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 3744-3747 [PMID:25052428]
ChEMBL Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay B 6.48 pEC50 330 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 3744-3747 [PMID:25052428]
Human herpesvirus 5 chemokine receptor in Human cytomegalovirus (strain AD169) (HHV-5) (Human herpesvirus 5) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4259] [UniProtKB: P69332]
ChEMBL Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay B 6.45 pEC50 354.81 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 3744-3747 [PMID:25052428]
ChEMBL Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay B 6.46 pEC50 350 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 3744-3747 [PMID:25052428]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 8.1 pKi - - - Eur. J. Pharmacol. (1998) 355: 245-56 [PMID:9760039];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 205-17 [PMID:9550290]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in membranes after 60 mins by microbeta scintillation counting method B 8.34 pKi 4.6 nM Ki Bioorg Med Chem Lett (2016) 26: 5315-5321 [PMID:27692547]
ChEMBL Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method B 8.4 pKi 4 nM Ki Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor B 8.66 pKi 2.2 nM Ki J. Med. Chem. (2003) 46: 265-283 [PMID:12519065]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.5 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 370: 114-23 [PMID:15322733]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2002) 45: 344-359 [PMID:11784139]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 8.4 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 370: 114-23 [PMID:15322733]
ChEMBL Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay F 9.42 pEC50 0.38 nM EC50 Eur. J. Med. Chem. (2013) 63: 558-569 [PMID:23537943]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity for rodent 5-hydroxytryptamine 5A receptor B 7 pKi 100 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 8.9 pKi - - - FEBS Lett. (1994) 355: 242-6 [PMID:7988681];
Eur. J. Pharmacol. (2001) 418: 157-67 [PMID:11343685]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 5A receptor B 9 pKi 1 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand B 9 pKi 1 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 7 pKi - - - Mol. Pharmacol. (1993) 43: 313-9 [PMID:8450829];
Eur. J. Pharmacol. (2001) 418: 157-67 [PMID:11343685]
5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364]
GtoPdb - - 7.5 pKi - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 3452-6 [PMID:7682702]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis B 8.39 pKi 4.1 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method B 8.39 pKi 4.1 nM Ki Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting B 9 pKi 1 nM Ki J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
ChEMBL Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 9.4 pKi - - - J. Neurochem. (1996) 66: 47-56 [PMID:8522988];
Mol Pharmacol (1998) 54: 577-583 [PMID:9730917];
Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]
ChEMBL Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay F 6.9 pIC50 127 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 738-743 [PMID:18053713]
ChEMBL Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation F 7.96 pIC50 11 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method B 8.33 pIC50 4.7 nM IC50 Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method F 8.33 pIC50 4.7 nM IC50 Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor by scintillation counting B 8.62 pIC50 2.4 nM IC50 J. Med. Chem. (2010) 53: 2521-2527 [PMID:20170099]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
ChEMBL Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting B 7 pKi 100 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 2333-2338 [PMID:26996373]
ChEMBL Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting B 7 pKi 100 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 2333-2338 [PMID:26996373]
ChEMBL Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting B 8.42 pKi 3.8 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 2333-2338 [PMID:26996373]
GtoPdb - - 9.4 pKi - - - Mol. Pharmacol. (1993) 43: 320-7 [PMID:7680751];
Neuropharmacology (1997) 36: 713-20 [PMID:9225298];
J. Neurochem. (1998) 71: 2169-77 [PMID:9798944];
Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor B 8.43 pKi 3.7 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method B 8.77 pKi 1.7 nM Ki Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting B 9 pKi 1 nM Ki J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
GtoPdb - - 9.4 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2001) 363: 620-32 [PMID:11414657];
Br. J. Pharmacol. (1997) 122: 126-32 [PMID:9298538];
J. Biol. Chem. (1993) 268: 23422-6 [PMID:8226867];
Br. J. Pharmacol. (1998) 124: 1300-6 [PMID:9720804]
ChEMBL Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay B 7.68 pIC50 21 nM IC50 Eur. J. Med. Chem. (2016) 112: 258-269 [PMID:26900658]
ChEMBL Displacement of [3H]LSD from human recombinant 5HT7 receptor B 8.51 pIC50 3.1 nM IC50 Bioorg. Med. Chem. (2008) 16: 2570-2578 [PMID:18083580]
ChEMBL Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation F 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells B 9.22 pEC50 0.6 nM EC50 J. Nat. Prod. (2006) 69: 432-435 [PMID:16562853]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 8.2 pKi - - - Mol. Pharmacol. (1993) 44: 229-36 [PMID:8394987]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 8.4 pKi 4 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 9.4 pKi - - - J. Biol. Chem. (1993) 268: 18200-4 [PMID:8394362]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 8.5 pKi - - - 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];
Eur. J. Pharmacol. (1996) 314: 365-72 [PMID:8957260]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 8.2 pKi - - - Eur. J. Pharmacol. (1996) 314: 365-72 [PMID:8957260];
Naunyn Schmiedebergs Arch. Pharmacol. (1997) 356: 328-34 [PMID:9303569];
Mol. Pharmacol. (1996) 50: 1567-80 [PMID:8967979];
Mol. Pharmacol. (1991) 40: 143-8 [PMID:1652050]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 7 pKi - - - J. Neurochem. (1996) 67: 2096-103 [PMID:8863519];
Proc. Natl. Acad. Sci. U.S.A. (1992) 89: 5517-21 [PMID:1608964];
Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 408-12 [PMID:8380639];
Eur. J. Pharmacol. (2004) 484: 127-39 [PMID:14744596]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 6.2 pKi - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 408-12 [PMID:8380639];
Neuropharmacology (1997) 36: 569-76 [PMID:9225282]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 9.2 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 370: 114-23 [PMID:15322733];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 17-24 [PMID:9459568]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]