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 33:
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]
