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ChEMBL ligand: CHEMBL69257 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Compound was evaluated for its ability to displace [3H]spiperone binding from Dopamine receptor D2 in rat striatum. | B | 6.98 | pKi | 104.71 | nM | Ki | J Med Chem (1999) 42: 533-535 [PMID:10052959] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Compound was evaluated for its ability to displace [3H]8-OH-DPAT binding from human 5-hydroxytryptamine 1A receptor in mammalian cells | B | 6.77 | pKi | 169.82 | nM | Ki | J Med Chem (1999) 42: 533-535 [PMID:10052959] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 6.77 | pKi | 169 | nM | Ki | Eur J Med Chem (2014) 85: 716-726 [PMID:25128671] |
ChEMBL | Antagonist activity at 5-HT1A receptor (unknown origin) | B | 6.77 | pKi | 169 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
ChEMBL | Compound was evaluated for its ability to displace [3H]GR-113808 binding from 5-hydroxytryptamine 4 receptor in guinea pig striatum. | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 533-535 [PMID:10052959] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor | B | 6.28 | pKi | 524.81 | nM | Ki | J Med Chem (1999) 42: 533-535 [PMID:10052959] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Binding affinity to 5HT7 receptor | B | 8.48 | pKi | 3.31 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1118-1123 [PMID:20022748] |
ChEMBL | Binding affinity to 5-HT7 receptor (unknown origin) | B | 8.67 | pKi | 2.14 | nM | Ki | J Med Chem (2018) 61: 8475-8503 [PMID:29767995] |
ChEMBL | Displacement of [3H]5-CT from recombinant human 5-HT7 receptor expressed in COS-7 cell membranes after 30 mins by liquid scintillation counting method | B | 8.67 | pKi | 2.14 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2418-2421 [PMID:29910079] |
ChEMBL | Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 8.67 | pKi | 2.14 | nM | Ki | Eur J Med Chem (2014) 85: 716-726 [PMID:25128671] |
ChEMBL | Displacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counter | B | 8.67 | pKi | 2.14 | nM | Ki | Bioorg Med Chem (2012) 20: 1545-1556 [PMID:22277589] |
ChEMBL | Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand | B | 8.67 | pKi | 2.14 | nM | Ki | J Med Chem (2002) 45: 2197-2206 [PMID:12014957] |
ChEMBL | Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells. | B | 8.67 | pKi | 2.14 | nM | Ki | J Med Chem (1999) 42: 533-535 [PMID:10052959] |
ChEMBL | Ability to displace the radioligand [3H]5-carboximidotryptamine ([3H]-5-CT) from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells | B | 8.67 | pKi | 2.14 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 61-64 [PMID:12467617] |
ChEMBL | Antagonist activity at 5-HT7 receptor (unknown origin) | B | 8.67 | pKi | 2.13 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2451-2454 [PMID:12161155] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki |
J Med Chem (1999) 42: 533-5 [PMID:10052959]; J Med Chem (2003) 46: 2795-812 [PMID:12825922] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand. | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
ChEMBL | Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand. | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
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]