RU 24969 [Ligand Id: 23] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL18785 (RU-24969)
  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • 7.96
1 CHEMBL18785_lig_chart_1 5-HT1A receptor HumanRat
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
  • 8.4
2 CHEMBL18785_lig_chart_2 5-HT1B receptor HumanRat
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
  • This target only has 1 pki data point
  • 7.7
3 CHEMBL18785_lig_chart_3 Serotonin 1d (5-HT1d) receptor Human
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 6.9
4 CHEMBL18785_lig_chart_4 Serotonin 2a (5-HT2a) receptor Human
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 6.6
5 CHEMBL18785_lig_chart_5 Serotonin 2c (5-HT2c) receptor Human
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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
  • 6.2
6 CHEMBL18785_lig_chart_6 Serotonin 6 (5-HT6) receptor Human
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
  • 7.8
7 CHEMBL18785_lig_chart_7 5-HT2B receptor HumanRat
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  • 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
  • 6.5
8 CHEMBL18785_lig_chart_8 5-HT5A receptor HumanMouse
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  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • This target only has 1 pki data point
  • 6.9
9 CHEMBL18785_lig_chart_9 5-HT7 receptor Mouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 9 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. B 7.96 pKi 10.96 nM Ki J. Med. Chem. (1993) 36: 4006-4014 [PMID:8258822]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 7.96 pKi 10.96 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Binding affinity to 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand assay. B 7.96 pKi 10.9 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 2963-2968
ChEMBL Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. B 8.3 pKi 5 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor B 7.85 pIC50 14 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Displacement of [3H]-8-OH-DPAT from rat 5HT1A receptor B 8.4 pIC50 4 nM IC50 Eur. J. Med. Chem. (2013) 63: 578-588 [PMID:23542166]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 8.1 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. B 8.4 pKi 4 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptor B 8.22 pIC50 6 nM IC50 Eur. J. Med. Chem. (2013) 63: 578-588 [PMID:23542166]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 7.7 pKi - - - Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]
ChEMBL Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1D receptor of bovine caudate using [3H]5-HT as the radioligand B 7.41 pIC50 39 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 6.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL Displacement of [3H]-ketanserin from human 5HT2A receptor B 6 pIC50 >1000 nM IC50 Eur. J. Med. Chem. (2013) 63: 578-588 [PMID:23542166]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. B 6.4 pKi 400 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
GtoPdb - - 6.8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL Displacement of [3H]-mesulergine from human 5HT2C receptor B 6.52 pIC50 300 nM IC50 Eur. J. Med. Chem. (2013) 63: 578-588 [PMID:23542166]
ChEMBL Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand B 6.54 pIC50 290 nM IC50 J. Med. Chem. (1990) 33: 2087-2093 [PMID:2374139]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 6.2 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]
ChEMBL Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells B 7.1 pIC50 79 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 3230-4234 [PMID:16055331]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 6.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 7.8 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
GtoPdb - - 6 pKi - - - FEBS Lett (1994) 355: 242-6 [PMID:7988681]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 6.5 pKi - - - Mol Pharmacol (1993) 43: 313-9 [PMID:8450829]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 6.9 pKi - - - Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]

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]