TFMPP [Ligand Id: 115] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL274866
  • 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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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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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-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
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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 Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against Dopamine receptor D1 B 6 pKi >1000 nM Ki J. Med. Chem. (1989) 32: 1052-1056 [PMID:2565400]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against Dopamine receptor D2 B 6.28 pKi 530 nM Ki J. Med. Chem. (1989) 32: 1052-1056 [PMID:2565400]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. B 5.71 pKi 1950 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain B 6.76 pKi 175 nM Ki J. Med. Chem. (1988) 31: 1968-1971 [PMID:3172131]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand. B 6.76 pKi 175 nM Ki J. Med. Chem. (1996) 39: 4439-4450 [PMID:8893838]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 6.76 pKi 173.78 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1A receptor B 7.09 pKi 80.6 nM Ki J. Med. Chem. (1989) 32: 1052-1056 [PMID:2565400]
ChEMBL Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor B 6.54 pIC50 290 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.9 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
J Neurochem (1996) 67: 2096-103 [PMID:8863519]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone. B 6.53 pKi 298 nM Ki J. Med. Chem. (1985) 28: 945-948 [PMID:4009617]
ChEMBL Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT B 6.94 pKi 116 nM Ki J. Med. Chem. (1985) 28: 945-948 [PMID:4009617]
ChEMBL Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. B 7.52 pKi 30 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor B 8.65 pKi 2.25 nM Ki J. Med. Chem. (1989) 32: 1052-1056 [PMID:2565400]
ChEMBL Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM B 7.29 pIC50 51 nM IC50 J. Med. Chem. (1989) 32: 720-727 [PMID:2537429]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT B 7.57 pIC50 27 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 7.2 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]
ChEMBL Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1D receptor of bovine caudate using [3H]5-HT as the radioligand B 6.21 pIC50 610 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 7.8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Synapse (2000) 35: 144-150 [PMID:10611640]
ChEMBL Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand B 6.82 pIC50 150 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
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: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
ChEMBL Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells B 5.86 pKi 1390 nM Ki J. Med. Chem. (1996) 39: 4017-4026 [PMID:8831767]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Binding affinity towards sigma receptor in guinea pig brain membranes using [3H]DTG as radioligand B 5.87 pKi 1340 nM Ki J. Med. Chem. (1991) 34: 3360-3365 [PMID:1662725]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 5.4 pKi - - - J Neurochem (1996) 67: 2096-103 [PMID:8863519];
Proc Natl Acad Sci USA (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 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 7.2 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 7.1 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 5.6 pKi - - - Mol Pharmacol (1993) 43: 313-9 [PMID:8450829]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 6.4 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 6.3 pKi - - - Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 6.3 pKi - - - Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 6.6 pKi - - - J Biol Chem (1993) 268: 18200-4 [PMID:8394362]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]