2-MPP [Ligand Id: 280] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL9666 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes | B | 5.45 | pKi | 3508 | nM | Ki | J Med Chem (1991) 34: 1850-1854 [PMID:1648138] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1992) 35: 743-750 [PMID:1347318] |
| Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833] | ||||||||
| ChEMBL | Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol | B | 4.47 | pIC50 | 34000 | nM | IC50 | J Med Chem (1992) 35: 743-750 [PMID:1347318] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Binding affinity at rat Dopamine receptor D1 by [3H]SCH-23390 displacement. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D2L receptor expressed in FlpIn CHO cell membrane after 3 hrs by liquid scintillation counting analysis | B | 5.39 | pKi | 4110 | nM | Ki | J Med Chem (2014) 57: 4924-4939 [PMID:24827597] |
| ChEMBL | Displacement of [3H]spiperone from human D2L receptor expressed in FlpIn CHO cell membrane after 3 hrs by liquid scintillation counting analysis | B | 5.39 | pKi | 4073.8 | nM | Ki | J Med Chem (2014) 57: 4924-4939 [PMID:24827597] |
| ChEMBL | Displacement of [125I]IABN from human D2L receptor expressed in HEK293 cells after 60 mins by gamma counting analysis | B | 6.17 | pKi | 679.6 | nM | Ki | J Med Chem (2012) 55: 6689-6699 [PMID:22632094] |
| ChEMBL | Antagonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of dopamine-induced ERK1/2 phosphorylation treated for 30 mins prior to dopamine stimulation for 5 mins by AlphaScreen assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2014) 57: 4924-4939 [PMID:24827597] |
| ChEMBL | Antagonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of dopamine-induced ERK1/2 phosphorylation treated for 30 mins prior to dopamine stimulation for 5 mins by AlphaScreen assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2014) 57: 4924-4939 [PMID:24827597] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro displacement of [3H]spiperone from Dopamine receptor D2 binding site in rat striatum. | B | 5.92 | pKi | 1200 | nM | Ki | J Med Chem (1997) 40: 300-312 [PMID:9022796] |
| ChEMBL | Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
| ChEMBL | Binding affinity against rat Dopamine receptor D2. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [125I]IABN from human D3 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis | B | 5.65 | pKi | 2262 | nM | Ki | J Med Chem (2012) 55: 6689-6699 [PMID:22632094] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor measured by displacing [3H]8-OH-DPAT from rat cortical membranes | B | 6.55 | pKi | 281 | nM | Ki | J Med Chem (1991) 34: 1850-1854 [PMID:1648138] |
| ChEMBL | Displacement of [3H]2-(di-N-propylamino)-8-hydroxytetralin from central 5-hydroxytryptamine 1A receptor recognition sites in rat frontal cortex homogenates. | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (1995) 38: 1942-1954 [PMID:7783126] |
| ChEMBL | Displacement of radioligand [3H]2-(di-N-propylamino)-8-hydroxytetralin from 5-hydroxytryptamine 1A receptor in rat frontal cortex homogenate | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (1993) 36: 2751-2760 [PMID:8410989] |
| ChEMBL | Binding affinity was evaluated by determining in vitro displacement of [3H]8-OH-DPAT from the central 5-hydroxytryptamine 1A receptor recognition site in rat frontal cortex homogenate. | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (1997) 40: 300-312 [PMID:9022796] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand. | B | 7.17 | pKi | 68 | nM | Ki | J Med Chem (1996) 39: 4439-4450 [PMID:8893838] |
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain | B | 7.17 | pKi | 68 | nM | Ki | J Med Chem (1988) 31: 1968-1971 [PMID:3172131] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 7.17 | pKi | 67.61 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 7.89 | pKi | 12.88 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 1A receptor by [3H]WB-4101 displacement. | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement. | B | 7.76 | pKi | 17.3 | 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 | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (1996) 39: 4017-4026 [PMID:8831767] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity against 5 Hydroxy tryptamine 6 receptor | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Displacement of [3H]LSD from rat kidney proximal convoluted tubule 5HT7R expressed in COS7 cells | B | 6.61 | pKi | 243 | nM | Ki | J Med Chem (2012) 55: 6375-6380 [PMID:22738316] |
| GtoPdb | - | - | 6.9 | pKi | - | - | - | J Biol Chem (1993) 268: 18200-4 [PMID:8394362] |
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 7 receptor. | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2003) 46: 5365-5374 [PMID:14640545] |
| 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 | 4.95 | pKi | 11200 | nM | Ki | J Med Chem (1991) 34: 3360-3365 [PMID:1662725] |
ChEMBL data shown on this page come from version 34:
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]
