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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 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]