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 |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 1D 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/5-hydroxytryptamine receptor 2C 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: 144-50 [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] |
| D1 receptor/D(1A) dopamine 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/D(2) dopamine 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-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 non-opioid intracellular receptor 1 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 36:
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]
