DR-4004 [Ligand Id: 8431] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL69257
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]