TFMPP [Ligand Id: 115] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL274866 |
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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: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| 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 32:
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]
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