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]
  • This target only has 1 pki data point
  • 6.98
1 CHEMBL69257_lig_chart_1 Dopamine D2 receptor Rat
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 6.77
2 CHEMBL69257_lig_chart_2 Serotonin 1a (5-HT1a) receptor Human
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
  • This target only has 1 pki data point
  • 6
3 CHEMBL69257_lig_chart_3 Serotonin 4 (5-HT4) receptor Guinea pig
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • This target only has 1 pki data point
  • 6.28
4 CHEMBL69257_lig_chart_4 Serotonin 6 (5-HT6) receptor Human
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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]
  • 7.3
5 CHEMBL69257_lig_chart_5 Serotonin 7 (5-HT7) receptor HumanRat
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]